DMP696 [Ligand Id: 3499] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL44698 (DMP-696) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| 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] |
| ChEMBL | Binding affinity to human CRF1 receptor assessed as inhibition constant | B | 8.77 | pKi | 1.7 | nM | Ki | Eur J Med Chem (2021) 223: 113537-113537 [PMID:34147747] |
| 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 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]
