R121919 [Ligand Id: 3520] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL309138 (R-121919)
  • 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]
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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 Binding affinity to recombinant human CRF1 receptor expressed in CHO cells B 9.52 pKd 0.3 nM Kd Bioorg. Med. Chem. Lett. (2011) 21: 6108-6111 [PMID:21889333]
ChEMBL Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation F 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6108-6111 [PMID:21889333]
ChEMBL Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation F 8.08 pKi 8.3 nM Ki J. Med. Chem. (2012) 55: 5255-5269 [PMID:22587443]
ChEMBL Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells B 8.11 pKi 7.8 nM Ki J. Med. Chem. (2005) 48: 4100-4110 [PMID:15943483]
ChEMBL Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells B 8.3 pKi 5 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 2133-2136 [PMID:12127521]
ChEMBL Antagonist activity at human recombinant CRF1 receptor F 8.4 pKi 3.98 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7259-7264 [PMID:21074436]
ChEMBL Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor B 8.46 pKi 3.5 nM Ki J. Med. Chem. (2004) 47: 4787-4798 [PMID:15341493]
ChEMBL Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin) B 8.52 pKi 3 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 5111-5114 [PMID:26456805]
ChEMBL Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells B 8.52 pKi 3 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4486-4490 [PMID:18672365]
ChEMBL Antagonist activity at human CRF-1 receptor F 8.52 pKi 3 nM Ki J. Med. Chem. (2011) 54: 4187-4206 [PMID:21618986]
ChEMBL Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting B 8.59 pKi 2.6 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 5111-5114 [PMID:26456805]
GtoPdb - - 9 pKi 1 nM Ki J Psychiatr Res (2000) 34: 171-81 [PMID:10867111]
ChEMBL Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method B 7.17 pIC50 67 nM IC50 Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
ChEMBL Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor F 7.3 pIC50 50 nM IC50 J. Med. Chem. (2005) 48: 5104-5107 [PMID:16078829]
ChEMBL Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor B 7.3 pIC50 50 nM IC50 J. Med. Chem. (2004) 47: 4787-4798 [PMID:15341493]
ChEMBL Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells B 7.55 pIC50 28.18 nM IC50 J. Med. Chem. (2008) 51: 7370-7379 [PMID:18989952]
ChEMBL Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method B 7.77 pIC50 17 nM IC50 Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
ChEMBL Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method B 8.07 pIC50 8.5 nM IC50 J. Med. Chem. (2016) 59: 2551-2566 [PMID:26901666]
ChEMBL Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay F 8.4 pIC50 4 nM IC50 J. Med. Chem. (2012) 55: 8450-8463 [PMID:22971011]
CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353]
ChEMBL Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting B 8.42 pKi 3.8 nM Ki J. Med. Chem. (2011) 54: 4187-4206 [PMID:21618986]

ChEMBL data shown on this page come from version 28:

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]