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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 |
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Kv7.2/Kv7.3 in Human [GtoPdb: 561, 562] [UniProtKB: O43526, O43525] | ||||||||
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: 561, 562] [UniProtKB: O88943, O88944] | ||||||||
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: 562, 561] [UniProtKB: O43525, O43526] | ||||||||
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]