XE991 [Ligand Id: 2596] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL342375 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of ERG in human HEK293 cells incubated for 1 hr by thallium flux assay | B | 4.49 | pIC50 | >32000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126681-126681 [PMID:31668424] |
| Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526] | ||||||||
| GtoPdb | - | - | 6.15 | pIC50 | 710 | nM | IC50 | Science (1998) 282: 1890-3 [PMID:9836639] |
| ChEMBL | Inhibition of Kv7.2 in human HEK293 cells incubated for 1 hr by thallium flux assay | B | 7.26 | pIC50 | 55 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126681-126681 [PMID:31668424] |
| Kv7.1 in Human [GtoPdb: 560] [UniProtKB: P51787] | ||||||||
| GtoPdb | - | - | 6.1 | pKd | 780 | nM | Kd | Mol Pharmacol (2000) 57: 1218-23 [PMID:10825393] |
| Kv7.4 in Human [GtoPdb: 563] [UniProtKB: P56696] | ||||||||
| GtoPdb | - | - | 5.3 | pIC50 | 5500 | nM | IC50 | Am J Physiol, Cell Physiol (2001) 280: C859-66 [PMID:11245603] |
| Kv7.5 in Human [GtoPdb: 564] [UniProtKB: Q9NR82] | ||||||||
| GtoPdb | - | - | 4.2 | pIC50 | 65000 | nM | IC50 | J Biol Chem (2000) 275: 24089-95 [PMID:10816588] |
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]
