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 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]