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 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]
