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 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]
