ChEMBL ligand: CHEMBL1086310
Transient receptor potential cation channel subfamily A member 1 in Rhesus macaque [ChEMBL: CHEMBL6066835] [UniProtKB: A0A1D5QMT1] 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 Mouse [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8] TRPA1/Transient receptor potential cation channel subfamily A member 1 in Rat [ChEMBL: CHEMBL5160] [GtoPdb: 485] [UniProtKB: Q6RI86] There should be some charts here, you may need to enable JavaScript!
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] There should be some charts here, you may need to enable JavaScript!
TRPV1/Transient receptor potential cation channel subfamily V member 1 in Human [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] There should be some charts here, you may need to enable JavaScript!
TRPV3/Transient receptor potential cation channel subfamily V member 3 in Human [ChEMBL: CHEMBL5522] [GtoPdb: 509] [UniProtKB: Q8NET8] There should be some charts here, you may need to enable JavaScript!
TRPV4/Transient receptor potential cation channel subfamily V member 4 in Human [ChEMBL: CHEMBL3119] [GtoPdb: 510] [UniProtKB: Q9HBA0] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Transient receptor potential cation channel subfamily A member 1 in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6066835] [UniProtKB: A0A1D5QMT1]
ChEMBL	Antagonist activity at full length rhesus monkey TRPA1 transfected in HEK293F cells assessed as blockade of MO-induced TRPA1 channel activation by measuring Ca2+ influx in presence of 120 uM MO by FLIPR calcium assay	B	5.14	pIC50	7300	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
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]
ChEMBL	Antagonist activity at full length human TRPA1 transfected in HEK293F cells assessed as blockade of MO-induced TRPA1 channel activation by measuring Ca2+ influx in presence of 30 uM MO by FLIPR calcium assay	B	5.13	pIC50	7400	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
ChEMBL	Antagonist activity at recombinant human TRPA1 expressed in HEK293F cells assessed as reduction in AITC-induced increase in intracellular Ca2+ level by FLIPR-based Ca2+ assay	B	5.16	pIC50	6900	nM	IC50	Pain (2011) 152: 1165-1172 [PMID:21402443]
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 TRPA1 (unknown origin)	B	5.21	pIC50	6200	nM	IC50	Pain (2011) 152: 1165-1172 [PMID:21402443]
ChEMBL	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of allyl isothiocyanate-induced increase in intracellular calcium level incubated for 1 hrs by FLIPR based analysis	B	5.21	pIC50	6200	nM	IC50	Pain (2011) 152: 1165-1172 [PMID:21402443]
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 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]
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]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075310] [GtoPdb: 485] [UniProtKB: Q8BLA8]
ChEMBL	Antagonist activity at full length mouse TRPA1 transfected in HEK293F cells assessed as blockade of MO-induced TRPA1 channel activation by measuring Ca2+ influx in presence of 30 uM MO by FLIPR calcium assay	B	5.17	pIC50	6800	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
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 full length rat TRPA1 transfected in HEK293F cells assessed as blockade of MO-induced TRPA1 channel activation by measuring Ca2+ influx in presence of 30 uM MO by FLIPR calcium assay	B	5.12	pIC50	7600	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
ChEMBL	Antagonist activity at rat TRPA1 expressed in HEK293F cells assessed as reduction in AITC-induced increase in intracellular Ca2+ level by FLIPR-based Ca2+ assay	B	5.16	pIC50	6900	nM	IC50	Pain (2011) 152: 1165-1172 [PMID:21402443]
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]
TRPV1/Transient receptor potential cation channel subfamily V member 1 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]
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]

ChEMBL data shown on this page come from version 36:

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]