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, GW-582892X, GW582892X, Potiga, Retigabine, Trobalt, WAY-143841)
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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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  • Kv7.2/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]
  • Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Rat [ChEMBL: CHEMBL5530] [GtoPdb: 561] [UniProtKB: O88943]
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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
Kv7.2/Kv7.3 in Human [GtoPdb: 561562] [UniProtKB: O43526O43525]
GtoPdb - - 5.6 pEC50 2500 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425];
Cell Res (2021) 31: 52-61 [PMID:32884139]
GtoPdb - - 6.2 pEC50 631 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425]
Kv7.2/Kv7.3/Potassium voltage-gated channel subfamily KQT member 2/member 3 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885622] [GtoPdb: 561562] [UniProtKB: O88943O88944]
ChEMBL Agonist activity at rat KCNQ2/3 channel expressed in CHO cells by patch clamp method B 5.38 pEC50 4150 nM EC50 J Med Chem (2021) 64: 5816-5837 [PMID:33929863]
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 Activation of Kv7.2/Kv7.3 channel (unknown origin) expressed in CHO cells assessed as slope of fluorescent signal by FluxOR fluorescent dye based assay B 4.95 pEC50 11200 nM EC50 J Med Chem (2022) 65: 11340-11364 [PMID:35972998]
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];
Cell Res (2021) 31: 52-61 [PMID:32884139]
ChEMBL Activation of Kv7.2/Kv7.3 channel (unknown origin) expressed in CHO cells at + 80 mV assessed as leftward shift change in half activation potential measured after 24 hrs by whole cell patch clamp based electrophysiological method B 5.6 pEC50 2500 nM EC50 J Med Chem (2022) 65: 11340-11364 [PMID:35972998]
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]
ChEMBL Agonist activity at Kv7.2 (unknown origin) assessed as shifting of voltage dependent activation to more negative potentials by SyncroPatch assay B 5.38 pEC50 4210 nM EC50 Bioorg Med Chem Lett (2022) 71: 128841-128841 [PMID:35671848]
GtoPdb - - 5.6 pEC50 2500 nM EC50 J Neurosci (2001) 21: 5535-45 [PMID:11466425];
Cell Res (2021) 31: 52-61 [PMID:32884139]
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]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5530] [GtoPdb: 561] [UniProtKB: O88943]
ChEMBL Agonist activity at rat KCNQ2 channel expressed in CHO cells by patch clamp method B 5.69 pEC50 2040 nM EC50 J Med Chem (2021) 64: 5816-5837 [PMID:33929863]
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 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]