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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]