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ChEMBL ligand: CHEMBL1098 (Anekain, Bucaine, Bupivacaine, Bupivacaine liposome, Exparel, Liposomal bupivacaine, LIQ-865, LIQ865, Marcaine, Posimir, Ropivacaine hydrochloride impurity, bupivacaine-, Sensorcaine, SKY-0402, SKY0402) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]