antalarmin [Ligand Id: 3489] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL296641 (Antalarmin) |
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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 recombinant CRF1 receptor expressed in CHO cells by cAMP assay | F | 7.49 | pKi | 32 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 723-728 [PMID:22104142] |
| ChEMBL | Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells | B | 8.51 | pKi | 3.1 | nM | Ki | J Med Chem (2005) 48: 5104-5107 [PMID:16078829] |
| ChEMBL | Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells | B | 8.51 | pKi | 3.1 | nM | Ki | J Med Chem (2005) 48: 4100-4110 [PMID:15943483] |
| ChEMBL | Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2005) 48: 5780-5793 [PMID:16134945] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Endocrinology (1996) 137: 5747-50 [PMID:8940412] |
| ChEMBL | Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells | B | 9.08 | pKi | 0.84 | nM | Ki | J Med Chem (1999) 42: 833-848 [PMID:10072681] |
| ChEMBL | Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis | B | 7.73 | pIC50 | 18.62 | nM | IC50 | Eur J Med Chem (2014) 78: 1-9 [PMID:24675175] |
| ChEMBL | Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method | B | 7.73 | pIC50 | 18.62 | nM | IC50 | Eur J Med Chem (2017) 138: 900-908 [PMID:28750312] |
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
| ChEMBL | Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum | B | 8.6 | pKi | 2.5 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 707-710 [PMID:10782669] |
| ChEMBL | Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2003) 46: 3559-3562 [PMID:12904058] |
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]
