ICA-27243 [Ligand Id: 7667] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL402146 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] | ||||||||
| ChEMBL | Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting | F | 4.39 | pIC50 | 41000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334] |
| Kv7.3/Kv7.5/Voltage-gated potassium channel KCNQ3/KCNQ5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883311] [GtoPdb: 562, 564] [UniProtKB: O43525, Q9NR82] | ||||||||
| ChEMBL | Activation of human Kv7.3/7.5 by patch clamp method | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 3793-3797 [PMID:30327146] |
| Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221348] [GtoPdb: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
| GtoPdb | - | - | 6.3 | pEC50 | - | - | - | Neurosci Lett (2009) 465: 138-42 [PMID:19733209] |
| ChEMBL | Activation of human Kv7.2/7.3 by patch clamp method | B | 6.34 | pEC50 | 460 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 3793-3797 [PMID:30327146] |
| ChEMBL | Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting | F | 6.42 | pEC50 | 380 | nM | EC50 | ACS Med Chem Lett (2011) 2: 481-484 [PMID:24900334] |
| Kv7.4/Voltage-gated potassium channel subunit Kv7.4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3576] [GtoPdb: 563] [UniProtKB: P56696] | ||||||||
| ChEMBL | Activation of human Kv7.4 by patch clamp method | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 3793-3797 [PMID:30327146] |
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]
