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 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]