2-APB [Ligand Id: 2433] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL169233 (2-Aminoethoxydiphenyl Borate, 2-(Diphenylboryloxy)Ethanamine)
  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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  • TRPM2/Transient receptor potential cation channel subfamily M member 2 in Human [ChEMBL: CHEMBL1250402] [GtoPdb: 494] [UniProtKB: O94759]
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  • TRPC3 in Human [GtoPdb: 488] [UniProtKB: Q13507]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
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  • TRPM3 in Human [GtoPdb: 495] [UniProtKB: Q9HCF6]
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  • TRPM6 in Human [GtoPdb: 498] [UniProtKB: Q9BX84]
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  • TRPM7 in Mouse [GtoPdb: 499] [UniProtKB: Q923J1]
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  • TRPM8 in Mouse [GtoPdb: 500] [UniProtKB: Q8R4D5]
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  • TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3]
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  • TRPV2 in Mouse [GtoPdb: 508] [UniProtKB: Q9WTR1]
  • TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • TRPV3 in Mouse [GtoPdb: 509] [UniProtKB: Q8K424]
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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 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]