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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) |
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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 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]