ChEMBL ligand: CHEMBL173443
sPLA2-1B/Phospholipase A2 group 1B in Human [ChEMBL: CHEMBL4426] [GtoPdb: 1416] [UniProtKB: P04054] There should be some charts here, you may need to enable JavaScript!
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] There should be some charts here, you may need to enable JavaScript!
TRPM2/Transient receptor potential cation channel subfamily M member 2 in Human [ChEMBL: CHEMBL1250402] [GtoPdb: 494] [UniProtKB: O94759] 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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
sPLA2-1B/Phospholipase A2 group 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4426] [GtoPdb: 1416] [UniProtKB: P04054]
ChEMBL	Inhibition of PLA2 (unknown origin) using soybean phosphatidylcholine as substrate preincubated for 30 mins followed incubated for 60 mins after substrate addition by microplate reader relative to control	B	4.66	pIC50	22000	nM	IC50	J Med Chem (2021) 64: 3976-3996 [PMID:33784097]
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
ChEMBL	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	B	4.55	pEC50	28183.83	nM	EC50	Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
ChEMBL	Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay	B	4.55	pEC50	28000	nM	EC50	Eur J Med Chem (2019) 170: 141-156 [PMID:30878828]
TRPM2/Transient receptor potential cation channel subfamily M member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250402] [GtoPdb: 494] [UniProtKB: O94759]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced intracellular calcium flux at 0 mV holding potential by whole cell patch clamp electrophysiology method	B	5.35	pIC50	4500	nM	IC50	J Nat Prod (2017) 80: 2741-2750 [PMID:29019677]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293 cells assessed as inhibition of H2O2-induced intracellular calcium level by patch clamp technique	B	5.77	pIC50	1700	nM	IC50	J Med Chem (2013) 56: 10079-10102 [PMID:24304219]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in H2O2-induced intracellular calcium flux after 30 mins by Fluo4-AM dye based fluorescence assay	B	5.77	pIC50	1700	nM	IC50	Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced channel currents by whole cell patch clamp electrophysiology method	B	5.77	pIC50	1700	nM	IC50	Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293T cells assessed as blocked of ADPR-activated current by whole cell patch clamp electrophysiology	B	5.77	pIC50	1700	nM	IC50	J Med Chem (2021) 64: 3976-3996 [PMID:33784097]
GtoPdb	-	-	5.8	pIC50	1700	nM	IC50	Br J Pharmacol (2006) 148: 264-73 [PMID:16604090]
ChEMBL	Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced channel currents treated extracellularly after 60 secs by whole cell patch clamp electrophysiology method	B	6.49	pIC50	320	nM	IC50	Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL	Inhibition of human TRPM8 expressed in HEK293 cells assessed as reduction in H2O2-induced intracellular calcium flux after 30 mins by Fluo4-AM dye based fluorescence assay	B	5.41	pIC50	3900	nM	IC50	Eur J Med Chem (2018) 152: 235-252 [PMID:29723786]
ChEMBL	Inhibition of human TRPM8 expressed in HEK293T cells assessed as blocked of menthol-activated current by whole cell patch clamp electrophysiology relative to control	B	5.41	pIC50	3900	nM	IC50	J Med Chem (2021) 64: 3976-3996 [PMID:33784097]

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]