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 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]
