ChEMBL ligand: CHEMBL593902

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!

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	4.25	pIC50	56400	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 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	5.04	pIC50	9100	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
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	5.35	pIC50	4466.84	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	5.4	pIC50	4000	nM	IC50	Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
GtoPdb	Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay	-	5.5	pIC50	3100	nM	IC50	Mol Pain (2007) 3: 40 [PMID:18086313]
ChEMBL	Antagonist activity at human TRPA1 expressed in CHO cells assessed as inhibition of CA-induced increase in calcium influx by Fluo-4 dye based FLIPR analysis in presence of 50 uM CA	B	5.51	pIC50	3100	nM	IC50	Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL	Antagonist activity at human TRPA1 channel expressed in CHO cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx	F	5.51	pIC50	3100	nM	IC50	J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
GtoPdb	Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay	-	5.51	pIC50	3100	nM	IC50	Mol Pain (2007) 3: 40 [PMID:18086313]
ChEMBL	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as [45]Ca2+ influx by microbeta plate count	F	5.55	pIC50	2800	nM	IC50	Bioorg Med Chem Lett (2010) 20: 276-279 [PMID:19945872]
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	5.66	pIC50	2200	nM	IC50	Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155]
ChEMBL	Antagonist activity at full length human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced intracellular Ca2+ flux in presence of 10 uM AITC by Fluo4-AM dye based fluorescence analysis	B	5.76	pIC50	1720	nM	IC50	Bioorg Med Chem (2024) 110: 117812-117812 [PMID:38941887]
ChEMBL	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of cinnamaldehyde-induced [45]Ca2+ influx by microbeta plate count	F	1.26	pA2	1.26	uM	pA2	Bioorg Med Chem Lett (2010) 20: 276-279 [PMID:19945872]
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	4.48	pIC50	33000	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
ChEMBL	Antagonist activity at mouse TRPA1 channel expressed in CHO cells assessed as inhibition of cinnamaldehyde-induced intracellular calcium influx	F	5.35	pIC50	4500	nM	IC50	J Med Chem (2010) 53: 5085-5107 [PMID:20356305]
GtoPdb	Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay	-	5.35	pIC50	4500	nM	IC50	Mol Pain (2007) 3: 40 [PMID:18086313]
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	4.4	pIC50	39900	nM	IC50	J Pharmacol Exp Ther (2012) 341: 360-368 [PMID:22319196]
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	5.47	pIC50	3400	nM	IC50	Bioorg Med Chem (2012) 20: 1690-1698 [PMID:22325155]

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]