ICA-27243 [Ligand Id: 7667] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL402146
  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
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  • Kv7.3/Kv7.2/Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) in Human [ChEMBL: CHEMBL2221348] [GtoPdb: 562561] [UniProtKB: O43525O43526]
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  • Kv7.4/Voltage-gated potassium channel subunit Kv7.4 in Human [ChEMBL: CHEMBL3576] [GtoPdb: 563] [UniProtKB: P56696]
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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: P15382P51787]
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: 562564] [UniProtKB: O43525Q9NR82]
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: 562561] [UniProtKB: O43525O43526]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]