(S)-N-[1-(3-morpholin-4-yl-phenyl)-ethyl]-3-phenyl-acrylamide [Ligand Id: 2600] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL317935
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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]
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  • Kv7.4 in Human [GtoPdb: 563] [UniProtKB: P56696]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511]
ChEMBL Inhibition of recombinant human Cytochrome P450 19A1 B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2003) 46: 3778-3781 [PMID:12930139]
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 - - 5.5 pEC50 - - - J Med Chem (2003) 46: 3197-200 [PMID:12852750];
Neuropharmacology (2006) 51: 1068-77 [PMID:16904708]
ChEMBL Effect on resting membrane potential in SH-SY5Y human neuroblastoma cells expressing native KCNQ channels F 6.16 pEC50 690 nM EC50 J. Med. Chem. (2003) 46: 3197-3200 [PMID:12852750]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2476] [GtoPdb: 561] [UniProtKB: O43526]
GtoPdb - - 5.5 pEC50 - - - J Med Chem (2003) 46: 3197-200 [PMID:12852750];
Neuropharmacology (2006) 51: 1068-77 [PMID:16904708]
ChEMBL Effective concentration against Potassium voltage gated channel KQT-like subfamily, member 2 expressed in HEK 293 cells B 5.52 pEC50 3000 nM EC50 J. Med. Chem. (2003) 46: 3778-3781 [PMID:12930139]
ChEMBL Effective concentration against Potassium voltage gated channel, KQT-like subfamily, member 2 expressed in SH-SY5Y human neuroblastoma cells B 6.16 pEC50 690 nM EC50 J. Med. Chem. (2003) 46: 3778-3781 [PMID:12930139]
Kv7.2/Voltage-gated potassium channel subunit Kv7.2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2985] [GtoPdb: 561] [UniProtKB: Q9Z351]
ChEMBL Induced current in Xenopus laevis oocytes expressing cloned mKCNQ2 channels F 5.22 pEC50 6000 nM EC50 J. Med. Chem. (2003) 46: 3197-3200 [PMID:12852750]
ChEMBL Whole-cell patch-clamp on recombinant mouse KCNQ2 channels expressed in HEK 293 cells at -40 mV F 5.48 pEC50 3280 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 5.49 pEC50 3200 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 5.49 pEC50 3200 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6188-6191 [PMID:24070783]
Kv7.4 in Human [GtoPdb: 563] [UniProtKB: P56696]
GtoPdb - - 5 pIC50 10400 nM IC50 Neuropharmacology (2006) 51: 1068-77 [PMID:16904708]

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]