antalarmin [Ligand Id: 3489] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL296641 (Antalarmin) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
