R121919 [Ligand Id: 3520] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL309138 (R-121919) |
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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 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]
