DMP696 [Ligand Id: 3499] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL44698 (DMP-696) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998] | ||||||||
| ChEMBL | Antagonist activity at human CRF-1 receptor | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 4187-4206 [PMID:21618986] |
| ChEMBL | Compound was tested for the binding affinity to human corticotropin releasing factor receptor | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2000) 43: 1641-1660 [PMID:10794681] |
| ChEMBL | Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1 | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2000) 43: 449-456 [PMID:10669572] |
| ChEMBL | Compound was tested for the binding affinity to human corticotropin releasing factor receptor | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2000) 43: 1641-1660 [PMID:10794681] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | J Med Chem (2000) 43: 449-56 [PMID:10669572] |
| ChEMBL | Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (2000) 43: 1641-1660 [PMID:10794681] |
| ChEMBL | Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane | B | 7.4 | pIC50 | 39.81 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5218-5221 [PMID:17629700] |
| ChEMBL | Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2008) 51: 7370-7379 [PMID:18989952] |
| ChEMBL | Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2008) 51: 7273-7286 [PMID:18975927] |
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
| ChEMBL | Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2009) 52: 3073-3083 [PMID:19361210] |
| ChEMBL | Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2009) 52: 4161-4172 [PMID:19552436] |
| ChEMBL | Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2184-2187 [PMID:27020524] |
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]
