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ChEMBL ligand: CHEMBL173443 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]