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

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ChEMBL ligand: CHEMBL1098 (Ropivacaine hydrochloride impurity, bupivacaine-, Anekain, LIQ-865, Exparel, Bupivacaine, Marcaine, LIQ865, SKY-0402, SKY0402, Sensorcaine)
  • 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]
  • This target only has 0 pki data point
  • 0
1 CHEMBL1098_lig_chart_1 Potassium channel subfamily K member 3 HumanRat
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  • K2P9.1/Potassium channel subfamily K member 9 in Rat [ChEMBL: CHEMBL4295] [GtoPdb: 520] [UniProtKB: Q9ES08]
  • This target only has 0 pki data point
  • 0
2 CHEMBL1098_lig_chart_2 Potassium channel subfamily K member 9 Rat
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  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1098_lig_chart_3 Kv1.5 Human
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  • Kv4.3 in Mouse [GtoPdb: 554] [UniProtKB: Q9Z0V1]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1098_lig_chart_4 Kv4.3 Mouse
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  • Nav1.5 in Human [GtoPdb: 582] [UniProtKB: Q14524]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1098_lig_chart_5 Nav1.5 Human
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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 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]