retigabine [Ligand Id: 2601] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL41355 (AWD-21360, AWD21-360, D-23129, Ezogabine, GKE-841, GW582892X, GW-582892X, Potiga, Retigabine, Trobalt, WAY-143841)
  • 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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  • Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526]
  • Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Mouse [ChEMBL: CHEMBL2985] [GtoPdb: 561] [UniProtKB: Q9Z351]
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  • Kv7.3/Voltage-gated potassium channel subunit Kv7.3 in Human [ChEMBL: CHEMBL2684] [GtoPdb: 562] [UniProtKB: O43525]
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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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  • Kv7.5/Voltage-gated potassium channel subunit Kv7.5 in Human [ChEMBL: CHEMBL2925] [GtoPdb: 564] [UniProtKB: Q9NR82]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
ChEMBL Agonist activity at human KCNQ2/3 expressed in HEK293 cells by FLIPR based thallium influx assay B 5.36 pEC50 4380 nM EC50 Bioorg Med Chem Lett (2019) 29: 126603-126603 [PMID:31416667]
GtoPdb - - 5.6 pEC50 2500 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
ChEMBL Activation of human Kv7.2/Kv7.3 expressed in CHO cells assessed as increase in channel current amplitude by whole cell patch clamp electrophysiology assay B 5.76 pEC50 1720 nM EC50 J Med Chem (2020) 63: 163-185 [PMID:31815462]
GtoPdb - - 6.2 pEC50 631 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
ChEMBL Activation of KCNQ2/Q3 expressed in CHO cells by atomic absorption Rb'+ efflux assay B 6.37 pEC50 430 nM EC50 Eur. J. Med. Chem. (2011) 46: 934-943 [PMID:21296466]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526]
GtoPdb - - 5.6 pEC50 2500 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
ChEMBL Activation of human Kv7.2 expressed in CHO cells assessed as increase in channel current amplitude by whole cell patch clamp electrophysiology assay B 6.03 pEC50 930 nM EC50 J Med Chem (2020) 63: 163-185 [PMID:31815462]
ChEMBL Activation of KCNQ2 (unknown origin) expressed in CHO cells at 10 uM after 10 mins by atomic absorption spectrophotometry-based Rb+ flow assay B 6.46 pEC50 350 nM EC50 Bioorg Med Chem Lett (2018) 28: 1731-1735 [PMID:29706422]
ChEMBL Channel opening activity at KCNQ2 (unknown origin) expressed in CHO cells after 10 mins by atomic absorption spectrophotometry-based Rb+ flow assay B 6.46 pEC50 350 nM EC50 Bioorg Med Chem Lett (2018) 28: 3004-3008 [PMID:30061030]
ChEMBL Activity at Kv 7.2 channel expressed in cloned CHO cells by [86Rb] efflux assay B 6.82 pEC50 <150 nM EC50 J. Med. Chem. (2007) 50: 2576-2582 [PMID:17489574]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2985] [GtoPdb: 561] [UniProtKB: Q9Z351]
ChEMBL Whole-cell patch-clamp on recombinant mouse KCNQ2 channels expressed in HEK 293 cells at -40 mV F 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 1991-1995 [PMID:15050644]
ChEMBL Effect on outward potassium currents in whole-cell patch clamp assay of HEK 293 cells expressing cloned mouse KCNQ2 channel at -40 mV F 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 363-366 [PMID:15603955]
ChEMBL Induction of mouse KCNQ2 expressed in HEK293 cells at -40 mV holding potential by whole-cell patch clamp assay B 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6188-6191 [PMID:24070783]
Kv7.3/Voltage-gated potassium channel subunit Kv7.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2684] [GtoPdb: 562] [UniProtKB: O43525]
ChEMBL Activation of human Kv7.3 expressed in CHO cells assessed as increase in channel current amplitude by whole cell patch clamp electrophysiology assay B 5.41 pEC50 3900 nM EC50 J Med Chem (2020) 63: 163-185 [PMID:31815462]
GtoPdb - - 6.2 pEC50 631 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
Kv7.4/Voltage-gated potassium channel subunit Kv7.4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3576] [GtoPdb: 563] [UniProtKB: P56696]
GtoPdb - - 5.2 pEC50 6310 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
ChEMBL Agonist activity at human KCNQ4 expressed in CHOK1 cells by whole cell patch clamp assay B 5.23 pEC50 5900 nM EC50 ACS Med Chem Lett (2019) 10: 27-33 [PMID:30655942]
Kv7.5/Voltage-gated potassium channel subunit Kv7.5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2925] [GtoPdb: 564] [UniProtKB: Q9NR82]
GtoPdb - - 5 pEC50 10000 nM EC50 Eur J Pharmacol (2002) 437: 129-37 [PMID:11890900]
ChEMBL Agonist activity at human KCNQ5 expressed in CHOK1 cells by whole cell patch clamp assay B 5.46 pEC50 3450 nM EC50 ACS Med Chem Lett (2019) 10: 27-33 [PMID:30655942]

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]