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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| 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: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
| 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 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]; 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] |
| Kv7.3/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 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]
