Record Information
Version2.0 (beta)
Creation Date2009-03-06 11:58:21 -0700
Update Date2014-10-31 13:49:17 -0600
Accession NumberT3D0242
Identification
Common NameMercuric chloride
ClassSmall Molecule
DescriptionMercuric chloride is one of the most toxic chemical compounds of mercury, due to its high solubility in water. It is most often used as a laboratory reagent, and occasionally used to form amalgams with metals.
Compound Type
  • Industrial/Workplace Toxin
  • Inorganic Compound
  • Mercury Compound
  • Pollutant
  • Synthetic Compound
Chemical Structure
Thumb
Synonyms
Synonym
Abavit b
Agrosan
Bichloride of mercury
Bichloride, mercury
Calo-clor
Calochlor
Dichloromercury
Emisan 6
Fungchex
HgCl2
Mercuric bichloride
Mercuric perchloride
Mercury (II ) chloride
Mercury (II) chloride
Mercury bichloride
Mercury chloride
Mercury chloride (2)
Mercury dichloride
Mercury perchloride
Mercury(2+) chloride
Mercury(2+) dichloride
Mercury(II) chloride
Perchloride of mercury
Sublimate
Sublimate, corrosive
Chemical FormulaCl2Hg
Average Molecular Mass271.500 g/mol
Monoisotopic Mass271.908 g/mol
CAS Registry Number7487-94-7
IUPAC Namedichloromercury
Traditional Namemercuric chloride
SMILESCl[Hg]Cl
InChI IdentifierInChI=1S/2ClH.Hg/h2*1H;/q;;+2/p-2
InChI KeyInChIKey=LWJROJCJINYWOX-UHFFFAOYSA-L
Chemical Taxonomy
KingdomInorganic Compounds
Super ClassMixed Metal/Non-metal Compounds
ClassTransition Metal Salts
Sub ClassTransition Metal Chlorides
Direct ParentTransition Metal Chlorides
Alternative ParentsNot Available
Substituents
  • Acyclic compound
  • Transition metal chloride
Molecular FrameworkAcyclic Compounds
External Descriptors
  • Inorganic Fungicides (kegg)
  • Mercury Coordination Entity (chebi)
Biological Properties
StatusDetected and Quantified
OriginExogenous
Cellular Locations
  • Cytoplasm
  • Extracellular
Biofluid Locations
  • Blood
  • Cerebrospinal Fluid (CSF)
  • Urine
Tissue LocationsNot Available
PathwaysNot Available
ApplicationsNot Available
Biological RolesNot Available
Chemical RolesNot Available
Physical Properties
StateSolid
AppearanceWhite crystals.
Experimental Properties
PropertyValue
Melting Point277°C
Boiling PointNot Available
Solubility69 mg/mL at 20 °C [SHIU,WY et al. (1990)]
LogPNot Available
Predicted Properties
PropertyValueSource
logP0.57ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area0 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity12.27 m3·mol-1ChemAxon
Polarizability7.27 Å3ChemAxon
Spectra
SpectraNot Available
Toxicity Profile
Route of ExposureOral (8) ; inhalation (8) ; dermal (8)
Mechanism of ToxicityHigh-affinity binding of the divalent mercuric ion to thiol or sulfhydryl groups of proteins is believed to be the major mechanism for the activity of mercury. Through alterations in intracellular thiol status, mercury can promote oxidative stress, lipid peroxidation, mitochondrial dysfunction, and changes in heme metabolism. Mercury is known to bind to microsomal and mitochondrial enzymes, resulting in cell injury and death. For example, mercury is known to inhibit aquaporins, halting water flow across the cell membrane. It also inhibits the protein LCK, which causes decreased T-cell signalling and immune system depression. Mercury is also believed to inhibit neuronal excitability by acting on the postsynaptic neuronal membrane. It also affects the nervous system by inhibiting protein kinase C and alkaline phosphatase, which impairs brain microvascular formation and function, as well as alters the blood-brain barrier. Mercury also produces an autoimmune response, likely by modification of major histocompatibility complex (MHC) class II molecules, self peptides, T-cell receptors, or cell-surface adhesion molecules. (8, 4, 5, 6)
MetabolismMercury is absorbed mainly via ingestion and inhalation, then distributed throughout the body via the bloodstream, where a portion binds to sulfhydryl groups on haemoglobin. Mercury can undergo oxidation to mercuric mercury, which takes place via the catalase-hydrogen peroxide pathway. The mercury atom is able to diffuse down the cleft in the catalase enzyme to reach the active site where the heme ring is located. Oxidation most likely occurs in all tissue, as the catalase hydrogen peroxide pathway is ubiquitous. Following oxidation, mercury tends to accumulate in the kidneys. Mercury is excreted mainly by exhalation and in the faeces. (2, 8)
Toxicity ValuesLD50: 1 mg/kg (Oral, Rat) (14) LD50: 5 mg/kg (Intraperitoneal, Mouse) (14) LD50: 14 mg/kg (Subcutaneous, Rat) (14)
Lethal Dose1 gram for an adult human (average for inorganic mercurials). (7)
Carcinogenicity (IARC Classification)3, not classifiable as to its carcinogenicity to humans. (12)
Uses/SourcesMercuric chloride is most often used as a laboratory reagent, and occasionally used to form an amalgam with metals. (13)
Minimum Risk LevelChronic Inhalation: 0.0002 mg/m3 (11)
Health EffectsMercury mainly affects the nervous system. Exposure to high levels of metallic, inorganic, or organic mercury can permanently damage the brain, kidneys, and developing fetus. Effects on brain functioning may result in irritability, shyness, tremors, changes in vision or hearing, and memory problems. Acrodynia, a type of mercury poisoning in children, is characterized by pain and pink discoloration of the hands and feet. Mercury poisoning can also cause Hunter-Russell syndrome and Minamata disease. (8)
SymptomsCommon symptoms include peripheral neuropathy (presenting as paresthesia or itching, burning or pain), skin discoloration (pink cheeks, fingertips and toes), edema (swelling), and desquamation (dead skin peels off in layers). (1)
TreatmentMercury poisoning is treated by immediate decontamination and chelation therapy using DMSA, DMPS, DPCN, or dimercaprol. (3)
Normal Concentrations
CompoundBiofluidStatusValueAgeSexConditionDetails
Mercury BloodDetected and Quantified0.007 +/- 0.0036 uMElderly (>65 years old)BothNormal Details
Mercury BloodDetected and Quantified0.00302(0.00153-0.00480) uMNot SpecifiedBothNormal Details
Mercury BloodDetected and Quantified0.00777(0.00431-0.01233) uMAdult (>18 years old)BothNormal Details
Mercury BloodDetected and Quantified0.0116 +/- 0.0055 uMAdult (>18 years old)BothNormal Details
Mercury BloodDetected and Quantified0.00518 (0.00477-0.00568) uMAdult (>18 years old)Not SpecifiedNormal Details
Mercury BloodDetected and Quantified0.00209 (0.00181-0.00241) uMChildren (1-13 years old)Not SpecifiedNormal Details
Mercury BloodDetected and Quantified0.0029 +/- 0.0029 uMAdult (>18 years old)BothNormal Details
Mercury Cerebrospinal Fluid (CSF)Detected and Quantified0.004 +/- 0.002 uMAdult (>18 years old)BothNormal Details
Mercury UrineDetected and Quantified0.003 +/- 0.004 umol/mmol creatinineAdult (>18 years old)BothNormal Details
Mercury UrineDetected and Quantified0.000286 (0.000256-0.000313) umol/mmol creatinineAdult (>18 years old)Not SpecifiedNormal Details
Mercury UrineDetected and Quantified0.000222 (0.000198-0.000248) umol/mmol creatinineChildren (1-13 years old)Not SpecifiedNormal Details
Mercury UrineDetected and Quantified0.00041 +/- 0.00034 umol/mmol creatinineAdult (>18 years old)BothNormal Details
Chloride ion BloodDetected and Quantified110000.0 +/- 4500.0 uMNewborn (0-30 days old)Not SpecifiedNormal Details
Chloride ion BloodDetected and Quantified103200.0 +/- 2640.0 uMInfant (0-1 year old)Not SpecifiedNormal Details
Chloride ion BloodDetected and Quantified103700.0 +/- 1900.0 uMAdult (>18 years old)BothNormal Details
Chloride ion Cerebrospinal Fluid (CSF)Detected and Quantified0.06 +/- 0.08 uMAdult (>18 years old)BothNormal Details
Chloride ion UrineDetected and Quantified8881.6 (5263.2-17763.2) umol/mmol creatinineAdult (>18 years old)BothNormal Details
Abnormal Concentrations
CompoundBiofluidStatusValueAgeSexConditionDetails
Mercury BloodDetected and Quantified0.019 +/- 0.012 uMAdult (>18 years old)BothMultiple sclerosis Details
Mercury BloodDetected and Quantified0.01 +/- 0.0083 uMAdult (>18 years old)BothParkinson's disease Details
Mercury BloodDetected and Quantified>3.5 uMAdult (>18 years old)BothAcute mercury poisoning Details
Mercury BloodDetected and Quantified1.2 (0.5-1.5) uMAdult (>18 years old)BothChronic mercury (vapor) poisoning Details
Mercury BloodDetected and Quantified0.0088 +/- 0.0039 uMElderly (>65 years old)BothAlzheimer's disease Details
Mercury UrineDetected and Quantified>0.3 umol/mmol creatinineAdult (>18 years old)BothChronic mercury (vapor) poisoning Details
DrugBank IDNot Available
HMDB IDNot Available
PubChem Compound ID24085
ChEMBL IDNot Available
ChemSpider ID22517
KEGG IDC13377
UniProt IDNot Available
OMIM ID
ChEBI ID31823
BioCyc IDNot Available
CTD IDD008627
Stitch IDMercuric chloride
PDB IDNot Available
ACToR ID826
Wikipedia LinkNot Available
References
Synthesis ReferenceNot Available
MSDST3D0242.pdf
General References
  1. Horowitz Y, Greenberg D, Ling G, Lifshitz M: Acrodynia: a case report of two siblings. Arch Dis Child. 2002 Jun;86(6):453. [12023189 ]
  2. Clarkson TW, Magos L: The toxicology of mercury and its chemical compounds. Crit Rev Toxicol. 2006 Sep;36(8):609-62. [16973445 ]
  3. Clifton JC 2nd: Mercury exposure and public health. Pediatr Clin North Am. 2007 Apr;54(2):237-69, viii. [17448359 ]
  4. Madsen KM, Christensen EI: Effects of mercury on lysosomal protein digestion in the kidney proximal tubule. Lab Invest. 1978 Feb;38(2):165-74. [203771 ]
  5. Ziemba SE, Menard SL, McCabe MJ Jr, Rosenspire AJ: T-cell receptor signaling is mediated by transient Lck activity, which is inhibited by inorganic mercury. FASEB J. 2009 Jun;23(6):1663-71. doi: 10.1096/fj.08-117283. Epub 2009 Jan 23. [19168706 ]
  6. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
  7. Baselt RC (2000). Disposition of Toxic Drugs and Chemicals in Man, 5th ed. Foster City, CA: Chemical Toxicology Institute.
  8. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
  9. Wikipedia. Mercury poisoning. Last Updated 8 March 2009. [Link]
  10. Wikipedia. Metallothionein. Last Updated 20 December 2008. [Link]
  11. ATSDR - Agency for Toxic Substances and Disease Registry (2001). Minimal Risk Levels (MRLs) for Hazardous Substances. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
  12. International Agency for Research on Cancer (2009). IARC Monographs on the Evaluation of Carcinogenic Risks to Humans. [Link]
  13. Wikipedia. Mercury(II) chloride. Last Updated 17 May 2009. [Link]
  14. The Physical and Theoretical Chemistry Laboratory of Oxford University (2006). Material Safety Data Sheet (MSDS) for mercury (II) chloride . [Link]
Gene Regulation
Up-Regulated Genes
GeneGene SymbolGene IDInteractionChromosomeDetails
Down-Regulated Genes
GeneGene SymbolGene IDInteractionChromosomeDetails

Targets

General Function:
Inorganic ion transport and metabolism
Specific Function:
This isozyme may play a role in skeletal mineralization
Gene Name:
ALPL
Uniprot ID:
P05186
Molecular Weight:
57304.4 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Carbohydrate transport and metabolism
Specific Function:
Forms a water-specific channel that provides the plasma membranes of red cells and kidney proximal tubules with high permeability to water, thereby permitting water to move in the direction of an osmotic gradient
Gene Name:
AQP1
Uniprot ID:
P29972
Molecular Weight:
28526.0 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Water channel required to promote glycerol permeability and water transport across cell membranes. May contribute to water transport in the upper portion of small intestine. Isoform 2 is not permeable to urea and glycerol.
Gene Name:
AQP10
Uniprot ID:
Q96PS8
Molecular Weight:
31762.97 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Aquaporins facilitate the transport of water and small neutral solutes across cell membranes (By similarity).
Gene Name:
AQP11
Uniprot ID:
Q8NBQ7
Molecular Weight:
30202.59 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in transporter activity
Specific Function:
Aquaporins facilitate the transport of water and small neutral solutes across cell membranes (By similarity).
Gene Name:
AQP12A
Uniprot ID:
Q8IXF9
Molecular Weight:
31474.21 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in transporter activity
Specific Function:
Aquaporins facilitate the transport of water and small neutral solutes across cell membranes (By similarity).
Gene Name:
AQP12B
Uniprot ID:
A6NM10
Molecular Weight:
31475.13 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a water-specific channel that provides the plasma membranes of renal collecting duct with high permeability to water, thereby permitting water to move in the direction of an osmotic gradient.
Gene Name:
AQP2
Uniprot ID:
P41181
Molecular Weight:
28837.17 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Water channel required to promote glycerol permeability and water transport across cell membranes. Acts as a glycerol transporter in skin and plays an important role in regulating SC (stratum corneum) and epidermal glycerol content. Involved in skin hydration, wound healing, and tumorigenesis. Provides kidney medullary collecting duct with high permeability to water, thereby permitting water to move in the direction of an osmotic gradient. Slightly permeable to urea and may function as a water and urea exit mechanism in antidiuresis in collecting duct cells. It may play an important role in gastrointestinal tract water transport and in glycerol metabolism (By similarity).
Gene Name:
AQP3
Uniprot ID:
Q92482
Molecular Weight:
31543.605 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Carbohydrate transport and metabolism
Specific Function:
Forms a water-specific channel. Osmoreceptor which regulates body water balance and mediates water flow within the central nervous system
Gene Name:
AQP4
Uniprot ID:
P55087
Molecular Weight:
34829.4 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a water-specific channel. Implicated in the generation of saliva, tears, and pulmonary secretions.
Gene Name:
AQP5
Uniprot ID:
P55064
Molecular Weight:
28291.89 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a water-specific channel that participates in distinct physiological functions such as glomerular filtration, tubular endocytosis and acid-base metabolism (By similarity).
Gene Name:
AQP6
Uniprot ID:
Q13520
Molecular Weight:
29370.215 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a channel for water and glycerol.
Gene Name:
AQP7
Uniprot ID:
O14520
Molecular Weight:
37231.325 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a water-specific channel; mercury-sensitive. Not permeable to glycerol or urea.
Gene Name:
AQP8
Uniprot ID:
O94778
Molecular Weight:
27381.01 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in water transport
Specific Function:
Forms a channel with a broad specificity. Mediates passage of a wide variety of non-charged solutes including carbamides, polyols, purines, and pyrimidines in a phloretin- and mercury-sensitive manner, whereas amino acids, cyclic sugars, Na(+), K(+), Cl(-), and deprotonated monocarboxylates are excluded. Also permeable to urea and glycerol.
Gene Name:
AQP9
Uniprot ID:
O43315
Molecular Weight:
31430.77 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in establishment of epithelial cell polarity
Specific Function:
Keratin-binding protein required for epithelial cell polarization. Involved in apical junction complex (AJC) assembly via its interaction with PARD3. Required for ciliogenesis.
Gene Name:
FBF1
Uniprot ID:
Q8TES7
Molecular Weight:
125445.19 Da
References
  1. Li Y, Yan XP, Chen C, Xia YL, Jiang Y: Human serum albumin-mercurial species interactions. J Proteome Res. 2007 Jun;6(6):2277-86. Epub 2007 May 10. [17489621 ]
General Function:
Carbohydrate transport and metabolism
Specific Function:
Water channel. May be responsible for regulating the osmolarity of the lens
Gene Name:
MIP
Uniprot ID:
P30301
Molecular Weight:
28121.5 Da
References
  1. Yukutake Y, Tsuji S, Hirano Y, Adachi T, Takahashi T, Fujihara K, Agre P, Yasui M, Suematsu M: Mercury chloride decreases the water permeability of aquaporin-4-reconstituted proteoliposomes. Biol Cell. 2008 Jun;100(6):355-63. doi: 10.1042/BC20070132. [18167118 ]
General Function:
Involved in protein serine/threonine kinase activity
Specific Function:
PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters
Gene Name:
PRKCA
Uniprot ID:
P17252
Molecular Weight:
76765.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein serine/threonine kinase activity
Specific Function:
This is a calcium-activated, phospholipid-dependent, serine- and threonine-specific enzyme. PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters. May be considered as a novel component of the NF-kappa-B signaling axis responsible for the survival and activation of B-cells after BCR cross-linking
Gene Name:
PRKCB
Uniprot ID:
P05771
Molecular Weight:
76870.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein serine/threonine kinase activity
Specific Function:
This is calcium-independent, phospholipid-dependent, serine- and threonine-specific enzyme. PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters. May play a role in antigen-dependent control of B-cell function
Gene Name:
PRKCD
Uniprot ID:
Q05655
Molecular Weight:
77478.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein serine/threonine kinase activity
Specific Function:
PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters
Gene Name:
PRKCE
Uniprot ID:
Q02156
Molecular Weight:
83675.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in signal transduction
Specific Function:
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in the regulation of cell differentiation in keratinocytes and pre-B cell receptor, mediates regulation of epithelial tight junction integrity and foam cell formation, and is required for glioblastoma proliferation and apoptosis prevention in MCF-7 cells. In keratinocytes, binds and activates the tyrosine kinase FYN, which in turn blocks epidermal growth factor receptor (EGFR) signaling and leads to keratinocyte growth arrest and differentiation. Associates with the cyclin CCNE1-CDK2-CDKN1B complex and inhibits CDK2 kinase activity, leading to RB1 dephosphorylation and thereby G1 arrest in keratinocytes. In association with RALA activates actin depolymerization, which is necessary for keratinocyte differentiation. In the pre-B cell receptor signaling, functions downstream of BLNK by up-regulating IRF4, which in turn activates L chain gene rearrangement. Regulates epithelial tight junctions (TJs) by phosphorylating occludin (OCLN) on threonine residues, which is necessary for the assembly and maintenance of TJs. In association with PLD2 and via TLR4 signaling, is involved in lipopolysaccharide (LPS)-induced RGS2 down-regulation and foam cell formation. Upon PMA stimulation, mediates glioblastoma cell proliferation by activating the mTOR pathway, the PI3K/AKT pathway and the ERK1-dependent phosphorylation of ELK1. Involved in the protection of glioblastoma cells from irradiation-induced apoptosis by preventing caspase-9 activation. In camptothecin-treated MCF-7 cells, regulates NF-kappa-B upstream signaling by activating IKBKB, and confers protection against DNA damage-induced apoptosis. Promotes oncogenic functions of ATF2 in the nucleus while blocking its apoptotic function at mitochondria. Phosphorylates ATF2 which promotes its nuclear retention and transcriptional activity and negatively regulates its mitochondrial localization.
Gene Name:
PRKCH
Uniprot ID:
P24723
Molecular Weight:
77827.96 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in synaptic transmission
Specific Function:
Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that plays diverse roles in neuronal cells and eye tissues, such as regulation of the neuronal receptors GRIA4/GLUR4 and GRIN1/NMDAR1, modulation of receptors and neuronal functions related to sensitivity to opiates, pain and alcohol, mediation of synaptic function and cell survival after ischemia, and inhibition of gap junction activity after oxidative stress. Binds and phosphorylates GRIA4/GLUR4 glutamate receptor and regulates its function by increasing plasma membrane-associated GRIA4 expression. In primary cerebellar neurons treated with the agonist 3,5-dihyidroxyphenylglycine, functions downstream of the metabotropic glutamate receptor GRM5/MGLUR5 and phosphorylates GRIN1/NMDAR1 receptor which plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. May be involved in the regulation of hippocampal long-term potentiation (LTP), but may be not necessary for the process of synaptic plasticity. May be involved in desensitization of mu-type opioid receptor-mediated G-protein activation in the spinal cord, and may be critical for the development and/or maintenance of morphine-induced reinforcing effects in the limbic forebrain. May modulate the functionality of mu-type-opioid receptors by participating in a signaling pathway which leads to the phosphorylation and degradation of opioid receptors. May also contributes to chronic morphine-induced changes in nociceptive processing. Plays a role in neuropathic pain mechanisms and contributes to the maintenance of the allodynia pain produced by peripheral inflammation. Plays an important role in initial sensitivity and tolerance to ethanol, by mediating the behavioral effects of ethanol as well as the effects of this drug on the GABA(A) receptors. During and after cerebral ischemia modulate neurotransmission and cell survival in synaptic membranes, and is involved in insulin-induced inhibition of necrosis, an important mechanism for minimizing ischemic injury. Required for the elimination of multiple climbing fibers during innervation of Purkinje cells in developing cerebellum. Is activated in lens epithelial cells upon hydrogen peroxide treatment, and phosphorylates connexin-43 (GJA1/CX43), resulting in disassembly of GJA1 gap junction plaques and inhibition of gap junction activity which could provide a protective effect against oxidative stress (By similarity). Phosphorylates p53/TP53 and promotes p53/TP53-dependent apoptosis in response to DNA damage.
Gene Name:
PRKCG
Uniprot ID:
P05129
Molecular Weight:
78447.23 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in ATP binding
Specific Function:
Calcium-independent, phospholipid-dependent, serine- and threonine-specific kinase. May play a role in the secretory response to nutrients. Involved in cell polarization processes and the formation of epithelial tight junctions. Implicated in the activation of several signaling pathways including Ras, c-Src and NF-kappa-B pathways. Functions in both pro- and anti-apoptotic pathways. Functions in the RAC1/ERK signaling required for transformed growth. Plays a role in microtubule dynamics through interaction with RAB2A and GAPDH and recruitment to vesicular tubular clusters (VTCs)
Gene Name:
PRKCI
Uniprot ID:
P41743
Molecular Weight:
68261.9 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein serine/threonine kinase activity
Specific Function:
PKC is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. PKC also serves as the receptor for phorbol esters, a class of tumor promoters
Gene Name:
PRKCQ
Uniprot ID:
Q04759
Molecular Weight:
81866.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in vesicle transport along microtubule
Specific Function:
Calcium- and diacylglycerol-independent serine/threonine-protein kinase that functions in phosphatidylinositol 3-kinase (PI3K) pathway and mitogen-activated protein (MAP) kinase cascade, and is involved in NF-kappa-B activation, mitogenic signaling, cell proliferation, cell polarity, inflammatory response and maintenance of long-term potentiation (LTP). Upon lipopolysaccharide (LPS) treatment in macrophages, or following mitogenic stimuli, functions downstream of PI3K to activate MAP2K1/MEK1-MAPK1/ERK2 signaling cascade independently of RAF1 activation. Required for insulin-dependent activation of AKT3, but may function as an adapter rather than a direct activator. Upon insulin treatment may act as a downstream effector of PI3K and contribute to the activation of translocation of the glucose transporter SLC2A4/GLUT4 and subsequent glucose transport in adipocytes. In EGF-induced cells, binds and activates MAP2K5/MEK5-MAPK7/ERK5 independently of its kinase activity and can activate JUN promoter through MEF2C. Through binding with SQSTM1/p62, functions in interleukin-1 signaling and activation of NF-kappa-B with the specific adapters RIPK1 and TRAF6. Participates in TNF-dependent transactivation of NF-kappa-B by phosphorylating and activating IKBKB kinase, which in turn leads to the degradation of NF-kappa-B inhibitors. In migrating astrocytes, forms a cytoplasmic complex with PARD6A and is recruited by CDC42 to function in the establishment of cell polarity along with the microtubule motor and dynein. In association with FEZ1, stimulates neuronal differentiation in PC12 cells. In the inflammatory response, is required for the T-helper 2 (Th2) differentiation process, including interleukin production, efficient activation of JAK1 and the subsequent phosphorylation and nuclear translocation of STAT6. May be involved in development of allergic airway inflammation (asthma), a process dependent on Th2 immune response. In the NF-kappa-B-mediated inflammatory response, can relieve SETD6-dependent repression of NF-kappa-B target genes by phosphorylating the RELA subunit at 'Ser-311'. Necessary and sufficient for LTP maintenance in hippocampal CA1 pyramidal cells. In vein endothelial cells treated with the oxidant peroxynitrite, phosphorylates STK11 leading to nuclear export of STK11, subsequent inhibition of PI3K/Akt signaling, and increased apoptosis.
Gene Name:
PRKCZ
Uniprot ID:
Q05513
Molecular Weight:
67659.335 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
Not Available
Uniprot ID:
A6NKZ8
Molecular Weight:
Not Available
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
Not Available
Uniprot ID:
Q99867
Molecular Weight:
Not Available
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain (By similarity)
Gene Name:
TUBA4B
Uniprot ID:
Q9H853
Molecular Weight:
27547.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein polymerization
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name:
TUBAL3
Uniprot ID:
A6NHL2
Molecular Weight:
49908.305 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA1A
Uniprot ID:
Q71U36
Molecular Weight:
50136.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA1B
Uniprot ID:
P68363
Molecular Weight:
50152.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA1C
Uniprot ID:
Q9BQE3
Molecular Weight:
49896.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA3C
Uniprot ID:
Q13748
Molecular Weight:
49960.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain (By similarity)
Gene Name:
TUBA3E
Uniprot ID:
Q6PEY2
Molecular Weight:
49917.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA4A
Uniprot ID:
P68366
Molecular Weight:
49925.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in cell structure
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBA8
Uniprot ID:
Q9NY65
Molecular Weight:
50094.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBB
Uniprot ID:
P07437
Molecular Weight:
49671.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBB1
Uniprot ID:
Q9H4B7
Molecular Weight:
50328.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain (By similarity)
Gene Name:
TUBB2A
Uniprot ID:
Q13885
Molecular Weight:
49908.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain (By similarity)
Gene Name:
TUBB2B
Uniprot ID:
Q9BVA1
Molecular Weight:
49954.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBB3
Uniprot ID:
Q13509
Molecular Weight:
50433.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBB4
Uniprot ID:
P04350
Molecular Weight:
49586.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain
Gene Name:
TUBB2C
Uniprot ID:
P68371
Molecular Weight:
49832.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in structural molecule activity
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha-chain (By similarity)
Gene Name:
TUBB6
Uniprot ID:
Q9BUF5
Molecular Weight:
49858.0 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein polymerization
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name:
TUBB8
Uniprot ID:
Q3ZCM7
Molecular Weight:
49775.655 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein polymerization
Specific Function:
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name:
Not Available
Uniprot ID:
A6NNZ2
Molecular Weight:
49572.265 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in GTP binding
Specific Function:
In the elongating spermatid it is associated with the manchette, a specialized microtubule system present during reshaping of the sperm head (By similarity)
Gene Name:
TUBD1
Uniprot ID:
Q9UJT1
Molecular Weight:
51033.9 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in GTP binding
Specific Function:
Not Available
Gene Name:
TUBE1
Uniprot ID:
Q9UJT0
Molecular Weight:
52931.4 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in GTP binding
Specific Function:
Tubulin is the major constituent of microtubules. Gamma tubulin is found at microtubule organizing centers (MTOC) such as the spindle poles or the centrosome, suggesting that it is involved in the minus-end nucleation of microtubule assembly
Gene Name:
TUBG1
Uniprot ID:
P23258
Molecular Weight:
51169.5 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein polymerization
Specific Function:
Tubulin is the major constituent of microtubules. The gamma chain is found at microtubule organizing centers (MTOC) such as the spindle poles or the centrosome. Pericentriolar matrix component that regulates alpha/beta chain minus-end nucleation, centrosome duplication and spindle formation (By similarity).
Gene Name:
TUBG2
Uniprot ID:
Q9NRH3
Molecular Weight:
51091.32 Da
References
  1. ATSDR - Agency for Toxic Substances and Disease Registry (2008). Toxicological profile for mercury. U.S. Public Health Service in collaboration with U.S. Environmental Protection Agency (EPA). [Link]
General Function:
Involved in protein kinase activity
Specific Function:
Tyrosine kinase that plays an essential role for the selection and maturation of developing T-cell in the thymus and in mature T-cell function. Is constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors and plays a key role in T-cell antigen receptor(TCR)-linked signal transduction pathways. Association of the TCR with a peptide antigen-bound MHC complex facilitates the interaction of CD4 and CD8 with MHC class II and class I molecules, respectively, and thereby recruits the associated LCK to the vicinity of the TCR/CD3 complex. LCK then phosphorylates tyrosines residues within the immunoreceptor tyrosines-based activation motifs (ITAMs) in the cytoplasmic tails of the TCRgamma chains and CD3 subunits, initiating the TCR/CD3 signaling pathway. In addition, contributes to signaling by other receptor molecules. Associates directly with the cytoplasmic tail of CD2, and upon engagement of the CD2 molecule, LCK undergoes hyperphosphorylation and activation. Also plays a role in the IL2 receptor-linked signaling pathway that controls T-cell proliferative response. Binding of IL2 to its receptor results in increased activity of LCK. Is expressed at all stages of thymocyte development and is required for the regulation of maturation events that are governed by both pre-TCR and mature alpha beta TCR
Gene Name:
LCK
Uniprot ID:
P06239
Molecular Weight:
57870.0 Da
References
  1. Ziemba SE, Menard SL, McCabe MJ Jr, Rosenspire AJ: T-cell receptor signaling is mediated by transient Lck activity, which is inhibited by inorganic mercury. FASEB J. 2009 Jun;23(6):1663-71. doi: 10.1096/fj.08-117283. Epub 2009 Jan 23. [19168706 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin
Gene Name:
OPRM1
Uniprot ID:
P35372
Molecular Weight:
44780.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.18 uMNVS_GPCR_hOpiate_muNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in dopamine receptor activity
Specific Function:
This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49294.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.19 uMNVS_GPCR_hDRD1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in alpha2-adrenergic receptor activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49523.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.23 uMNVS_GPCR_hAdra2CNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in delta-opioid receptor activity
Specific Function:
Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins
Gene Name:
OPRD1
Uniprot ID:
P41143
Molecular Weight:
40413.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.26 uMNVS_GPCR_hOpiate_D1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in beta1-adrenergic receptor activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51323.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.30 uMNVS_GPCR_hAdrb1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
Receptor for the neuropeptide nociceptin/orphanin FQ. Has a potential role in modulating a number of brain functions, including instinctive behaviors and emotions. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase
Gene Name:
OPRL1
Uniprot ID:
P41146
Molecular Weight:
40694.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.31 uMNVS_GPCR_hORL1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in dopamine receptor activity
Specific Function:
This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50620.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.35 uMNVS_GPCR_hDRD2sNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Gene Name:
CHRM5
Uniprot ID:
P08912
Molecular Weight:
60074.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.35 uMNVS_GPCR_hM5Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in neurotransmitter:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69333.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.36 uMNVS_TR_hNETNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Gene Name:
CHRM3
Uniprot ID:
P20309
Molecular Weight:
66129.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.49 uMNVS_GPCR_hM3Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Secondary metabolites biosynthesis, transport and catabolism
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.5 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.80 uMNVS_ADME_hCYP2C19Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53556.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.83 uMNVS_GPCR_h5HT7Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in DNA binding
Specific Function:
Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis
Gene Name:
PPARG
Uniprot ID:
P37231
Molecular Weight:
57621.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.86 uMTox21_PPARg_BLA_Agonist_ratioTox21/NCGC
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in beta2-adrenergic receptor activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46557.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.92 uMNVS_GPCR_hAdrb2Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system
Gene Name:
HRH1
Uniprot ID:
P35367
Molecular Weight:
55785.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.94 uMNVS_GPCR_hH1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in xenobiotic metabolic process
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide.
Gene Name:
CYP3A4
Uniprot ID:
P05184
Molecular Weight:
57342.67 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC500.99 uMNVS_ADME_hCYP3A4Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in monooxygenase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58295.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.04 uMNVS_ADME_hCYP1A2Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
Gene Name:
CHRM1
Uniprot ID:
P11229
Molecular Weight:
51421.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.10 uMNVS_GPCR_hM1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51716.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.10 uMNVS_GPCR_hM2Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in DNA binding
Specific Function:
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Activated, but not phosphorylated, by HIPK3
Gene Name:
AR
Uniprot ID:
P10275
Molecular Weight:
98990.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.45 uMTox21_AR_BLA_Agonist_ratioTox21/NCGC
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in serotonin receptor signaling pathway
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins.
Gene Name:
HTR5A
Uniprot ID:
P47898
Molecular Weight:
40254.69 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.54 uMNVS_GPCR_h5HT5ANovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Cell cycle control, cell division, chromosome partitioning
Specific Function:
This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
Gene Name:
DRD4
Uniprot ID:
P21917
Molecular Weight:
48361.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.55 uMNVS_GPCR_hDRD4.4Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs
Gene Name:
HTR6
Uniprot ID:
P50406
Molecular Weight:
46955.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC501.61 uMNVS_GPCR_h5HT6Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in alpha2-adrenergic receptor activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48957.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC502.25 uMNVS_GPCR_hAdra2ANovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Secondary metabolites biosynthesis, transport and catabolism
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55770.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC502.45 uMNVS_ADME_hCYP2D6Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in endothelin receptor activity
Specific Function:
Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. The rank order of binding affinities for ET-A is:ET1 > ET2 >> ET3
Gene Name:
EDNRA
Uniprot ID:
P25101
Molecular Weight:
48723.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC502.96 uMNVS_GPCR_hETANovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Not Available
Specific Function:
This is a receptor for the tachykinin neuropeptide substance K (neurokinin A). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system
Gene Name:
TACR2
Uniprot ID:
P21452
Molecular Weight:
44440.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC503.41 uMNVS_GPCR_hNK2Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in DNA binding
Specific Function:
Receptor for glucocorticoids (GC). Has a dual mode of action:as a transcription factor that binds to glucocorticoid response elements (GRE) and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth
Gene Name:
NR3C1
Uniprot ID:
P04150
Molecular Weight:
85660.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC503.49 uMNVS_NR_hGRNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in monooxygenase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55629.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC503.55 uMNVS_ADME_hCYP2C9Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in nucleoside transmembrane transporter activity
Specific Function:
Mediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive (ES) to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (NBMPR) and is sodium-independent. It has a higher affinity for adenosine. Inhibited by dipyridamole and dilazep (anticancer chemotherapeutics drugs)
Gene Name:
SLC29A1
Uniprot ID:
Q99808
Molecular Weight:
50220.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC505.01 uMNVS_TR_hAdoTNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in A2A adenosine receptor activity, G-protein coupled
Specific Function:
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
Gene Name:
ADORA2A
Uniprot ID:
P29274
Molecular Weight:
44708.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC505.16 uMNVS_GPCR_hAdoRA2aNovascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase
Gene Name:
CHRM4
Uniprot ID:
P08173
Molecular Weight:
53050.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC505.50 uMNVS_GPCR_hM4Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Secondary metabolites biosynthesis, transport and catabolism
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.8 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC507.00 uMNVS_ADME_hCYP2B6Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in rhodopsin-like receptor activity
Specific Function:
Receptor for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PYY > NPY > PYY (3-36) > NPY (2-36) > [Ile-31, Gln-34] PP > [Leu- 31, Pro-34] NPY > PP, [Pro-34] PYY and NPY free acid
Gene Name:
NPY2R
Uniprot ID:
P49146
Molecular Weight:
42732.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC507.83 uMNVS_GPCR_hNPY2Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in angiotensin type II receptor activity
Specific Function:
Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
Gene Name:
AGTR1
Uniprot ID:
P30556
Molecular Weight:
41062.0 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC509.83 uMNVS_GPCR_hAT1Novascreen
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]
General Function:
Involved in transcription from RNA polymerase II promoter
Specific Function:
Transcription activator that binds to antioxidant response (ARE) elements in the promoter regions of target genes. Important for the coordinated up-regulation of genes in response to oxidative stress. May be involved in the transcriptional activation of genes of the beta-globin cluster by mediating enhancer activity of hypersensitive site 2 of the beta-globin locus control region.
Gene Name:
NFE2L2
Uniprot ID:
Q16236
Molecular Weight:
67825.9 Da
Binding/Activity Constants
TypeValueAssay TypeAssay Source
AC509.91 uMATG_NRF2_ARE_CISAttagene
References
  1. Sipes NS, Martin MT, Kothiya P, Reif DM, Judson RS, Richard AM, Houck KA, Dix DJ, Kavlock RJ, Knudsen TB: Profiling 976 ToxCast chemicals across 331 enzymatic and receptor signaling assays. Chem Res Toxicol. 2013 Jun 17;26(6):878-95. doi: 10.1021/tx400021f. Epub 2013 May 16. [23611293 ]