DMP696 [Ligand Id: 3499] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL44698 (DMP-696)
  • CRF1 receptor/Corticotropin releasing factor receptor 1 in Human [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998]
  • CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353]
1 CHEMBL44698_lig_chart_1 Corticotropin releasing factor receptor 1 HumanRat
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]