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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 |
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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 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]