2-APB [Ligand Id: 2433] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL169233 (2-Aminoethoxydiphenyl Borate, 2-(Diphenylboryloxy)Ethanamine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
| ChEMBL | Inhibition of rabbit skeletal muscle microsomes FITC-labelled SERCA1a incubated for 1 hr by fluorescence spectrophotometric method | B | 4.15 | pIC50 | 70000 | nM | IC50 | J Med Chem (2020) 63: 1937-1963 [PMID:32030976] |
| 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 HEK293T cells cotransfected with GFP assessed as reduction in ADPR-induced current by whole cell patch-clamp method | B | 5.3 | pIC50 | 5000 | nM | IC50 | Eur J Med Chem (2021) 225: 113750-113750 [PMID:34416664] |
| ChEMBL | Inhibition of human TRPM2 expressed in HEK293T cells assessed as blocked of ADPR-activated current by whole cell patch clamp electrophysiology | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2021) 64: 3976-3996 [PMID:33784097] |
| ChEMBL | Inhibition of human TRPM2 expressed in HEK293 cells | B | 5.92 | pIC50 | 1200 | nM | IC50 | Eur J Med Chem (2021) 225: 113750-113750 [PMID:34416664] |
| ChEMBL | Inhibition of human TRPM2 expressed in HEK293 cells | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2013) 56: 10079-10102 [PMID:24304219] |
| ChEMBL | Inhibition of human TRPM2 expressed in HEK293 cells assessed as reduction in ADPR-induced intracellular calcium flux by whole cell patch clamp electrophysiology method | B | 6 | pIC50 | 1000 | nM | IC50 | J Nat Prod (2017) 80: 2741-2750 [PMID:29019677] |
| GtoPdb | - | - | 6.1 | pIC50 | 820 | nM | IC50 | Br J Pharmacol (2008) 153: 1324-30 [PMID:18204483] |
| TRPC3 in Human [GtoPdb: 488] [UniProtKB: Q13507] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | 10000 | nM | IC50 | Mol Pharmacol (2005) 68: 758-62 [PMID:15933213] |
| TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 4.7 | pIC50 | 20000 | nM | IC50 | Br J Pharmacol (2005) 145: 405-14 [PMID:15806115] |
| TRPM3 in Human [GtoPdb: 495] [UniProtKB: Q9HCF6] | ||||||||
| GtoPdb | - | - | 4 | pIC50 | - | - | - | Br J Pharmacol (2005) 145: 405-14 [PMID:15806115] |
| TRPM6 in Human [GtoPdb: 498] [UniProtKB: Q9BX84] | ||||||||
| GtoPdb | - | - | 3.7 | pEC50 | 205000 | nM | EC50 | J Gen Physiol (2006) 127: 525-37 [PMID:16636202] |
| TRPM7 in Mouse [GtoPdb: 499] [UniProtKB: Q923J1] | ||||||||
| GtoPdb | - | - | 3.75 | pIC50 | 178000 | nM | IC50 | J Gen Physiol (2006) 127: 525-37 [PMID:16636202] |
| TRPM8 in Mouse [GtoPdb: 500] [UniProtKB: Q8R4D5] | ||||||||
| GtoPdb | - | - | 5.1 | pIC50 | - | - | - |
J Biol Chem (2004) 279: 35741-8 [PMID:15194687]; Neurochem Res (2012) 37: 314-20 [PMID:21964764] |
| TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3] | ||||||||
| GtoPdb | - | - | 3.9 | pEC50 | - | - | - | J Biol Chem (2004) 279: 35741-8 [PMID:15194687] |
| TRPV2 in Mouse [GtoPdb: 508] [UniProtKB: Q9WTR1] | ||||||||
| GtoPdb | - | - | 3.9 | pEC50 | 129000 | nM | EC50 |
J Biol Chem (2004) 279: 35741-8 [PMID:15194687]; Mol Pharmacol (2007) 72: 1258-68 [PMID:17673572] |
| TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
| GtoPdb | - | - | 5 | pEC50 | 10000 | nM | EC50 |
J Biol Chem (2007) 282: 15894-902 [PMID:17395593]; J Neurosci (2008) 28: 6231-8 [PMID:18550765] |
| TRPV3 in Mouse [GtoPdb: 509] [UniProtKB: Q8K424] | ||||||||
| GtoPdb | Patch clamp electrophysiology | - | 4.6 | pEC50 | 25100 | nM | EC50 | J Neurosci (2004) 24: 5177-82 [PMID:15175387] |
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]
