7-fluorochromone-2-carboxamide [Ligand Id: 1303] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL214021 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of 3H-dofetilide from hERG-expressing HEK membrane homogenates | B | 4.82 | pIC50 | 15100 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 874-878 [PMID:17234405] |
| ChEMBL | Displacement of [3H]dofetilide from hERG expressed in HEK293 cell membrane | B | 4.82 | pIC50 | 15100 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2365-2371 [PMID:17350253] |
| ChEMBL | Activity at hERG expressed in HEK293 cells assessed as blockade of current at -50 mV by voltage clamp assay | F | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2006) 49: 6569-6584 [PMID:17064075] |
| ChEMBL | Displacement of [3H]dofetilide from hERG | B | 7.82 | pIC50 | 15.1 | nM | IC50 | J Med Chem (2006) 49: 6569-6584 [PMID:17064075] |
| MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705] | ||||||||
| ChEMBL | Antagonist activity at MCHr1 assessed as inhibition of MCH-mediated calcium ion release in intact IMR32 cells by FLIPR assay | F | 7.54 | pIC50 | 29 | nM | IC50 | J Med Chem (2006) 49: 6569-6584 [PMID:17064075] |
| ChEMBL | Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells | F | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2365-2371 [PMID:17350253] |
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - | J Med Chem (2006) 49: 6569-84 [PMID:17064075] |
| ChEMBL | Displacement of [125I]MCH from MCHr1 expressed in IMR32 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2006) 49: 6569-6584 [PMID:17064075] |
| ChEMBL | Displacement of 125I-MCH from MCH-R1 expressed in IMR-32 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 874-878 [PMID:17234405] |
| ChEMBL | Displacement of [125I]MCH from MCHR1 expressed in IMR32 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 2365-2371 [PMID:17350253] |
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]
