HC030031 [Ligand Id: 4211] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1086310
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
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  • TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8]
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  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy B 4.74 pIC50 18000 nM IC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy B 4.75 pIC50 17782.79 nM IC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2012) 22: 797-800 [PMID:22222037]
ChEMBL Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx by FLIPR F 5.12 pIC50 7500 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
GtoPdb Calcium imaging - 5.2 pIC50 - - - Proc Natl Acad Sci USA (2007) 104: 13525-30 [PMID:17686976]
ChEMBL Antagonist activity at human TRPA1 channel assessed as inhibition of allyl isothiocyanate-induced intracellular calcium influx F 5.21 pIC50 6200 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
ChEMBL Inhibition of human TRPA1 expressed in HEK293 cells after 10 mins by FLIPR assay B 5.21 pIC50 6200 nM IC50 J Med Chem (2013) 56: 593-624 [PMID:23121096]
ChEMBL Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced increase in calcium influx by fluorescence analysis in presence of 5 uM AITC B 5.21 pIC50 6200 nM IC50 Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL Antagonist activity at human TRPA1 channel assessed as inhibition of formalin-induced intracellular calcium influx F 5.28 pIC50 5300 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
ChEMBL Antagonist activity at human TRPA1 channel expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx by FLIPR F 5.31 pIC50 4900 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
ChEMBL Antagonist activity at TRPA1 (unknown origin) B 5.64 pIC50 2300 nM IC50 J Med Chem (2014) 57: 5129-5140 [PMID:24884675]
ChEMBL Antagonist activity at human TRPA1 channel assessed as inhibition of nifedipine-induced intracellular calcium influx F 5.74 pIC50 1800 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
ChEMBL Antagonist activity at human TRPA1 expressed in human IMR90 cells assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis F 5.74 pIC50 1800 nM IC50 Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86]
ChEMBL Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of BITC-induced increase in intracellular calcium concentration by Fluo4-AM based fluorometric assay F 5.25 pIC50 5600 nM IC50 Bioorg Med Chem Lett (2012) 22: 797-800 [PMID:22222037]
ChEMBL Antagonist activity at Sprague-Dawley rat TRPA1 expressed in rat DRG neurons assessed as inhibition of acrolein-induced calcium influx after 40 mins by fluorescence analysis F 5.68 pIC50 2100 nM IC50 Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL Antagonist activity at human TRPM8 channel F 4.52 pIC50 >30000 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8]
ChEMBL Antagonist activity at human TRPV3 channel F 5 pIC50 >10000 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0]
ChEMBL Antagonist activity at human TRPV4 channel F 5 pIC50 >10000 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Antagonist activity at human TRPV1 channel F 4.7 pIC50 >20000 nM IC50 J Med Chem (2010) 53: 5085-5107 [PMID:20356305]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]