(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: 562, 561] [UniProtKB: O43525, O43526]
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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: 562, 561] [UniProtKB: O43525, O43526]
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 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]