antalarmin [Ligand Id: 3489] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL296641 (Antalarmin)
  • 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]
1 CHEMBL296641_lig_chart_1 Corticotropin releasing factor receptor 1 HumanRat
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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 27:

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]