bupivacaine [Ligand Id: 2397] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1098 (Anekain, Bucaine, Bupivacaine, Bupivacaine liposome, Exparel, Exparel liposomal, Liposomal bupivacaine, LIQ-865, LIQ865, Marcaine, Posimir, Ropivacaine hydrochloride impurity, bupivacaine-, Sensorcaine, SKY-0402, SKY0402)
  • K2P3.1/Potassium channel subfamily K member 3 in Human [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
  • K2P3.1/Potassium channel subfamily K member 3 in Rat [ChEMBL: CHEMBL4294] [GtoPdb: 515] [UniProtKB: O54912]
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  • K2P9.1/Potassium channel subfamily K member 9 in Rat [ChEMBL: CHEMBL4295] [GtoPdb: 520] [UniProtKB: Q9ES08]
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  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
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  • Kv4.3 in Mouse [GtoPdb: 554] [UniProtKB: Q9Z0V1]
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  • Nav1.5 in Human [GtoPdb: 582] [UniProtKB: Q14524]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
K2P3.1/Potassium channel subfamily K member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
ChEMBL Inhibition of human TASK1 expressed in Xenopus oocytes by whole cell voltage clamp assay B 4.39 pIC50 41000 nM IC50 J Med Chem (2019) 62: 10044-10058 [PMID:31260312]
K2P3.1/Potassium channel subfamily K member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4294] [GtoPdb: 515] [UniProtKB: O54912]
ChEMBL Inhibition of rat TASK1 expressed in African green monkey COS7 cells by outside-out patches based electrophysiology assay B 4.39 pIC50 41000 nM IC50 J Med Chem (2019) 62: 10044-10058 [PMID:31260312]
K2P9.1/Potassium channel subfamily K member 9 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295] [GtoPdb: 520] [UniProtKB: Q9ES08]
ChEMBL Inhibition of rat TASK3 expressed in African green monkey COS7 cells by outside-out patches based electrophysiology assay B 4 pIC50 100000 nM IC50 J Med Chem (2019) 62: 10044-10058 [PMID:31260312]
Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb - - 5.4 pKd - - - Circ Res (1997) 81: 1053-64 [PMID:9400387]
Kv4.3 in Mouse [GtoPdb: 554] [UniProtKB: Q9Z0V1]
GtoPdb - - 4 pIC50 - - - Am J Physiol Heart Circ Physiol (2007) 292: H2364-77 [PMID:17220193]
GtoPdb - - 4.5 pIC50 - - - Br J Pharmacol (2006) 149: 676-86 [PMID:17016508]
Nav1.5 in Human [GtoPdb: 582] [UniProtKB: Q14524]
GtoPdb - - 4.16 pIC50 69500 nM IC50 Anesth Analg (2015) 120: 1226-34 [PMID:25692452]
GtoPdb - - 5.66 pIC50 2180 nM IC50 Anesth Analg (2015) 120: 1226-34 [PMID:25692452]

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]