ChEMBL ligand: CHEMBL593902

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
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	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 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]
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]
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 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 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 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 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]