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Scintillation Proximity Assay from WIPO Patent WO2023285347: "NOVEL FATTY ACID MODIFIED UROCORTIN 2 DERIVATIVES AND THE USES THEREOF"
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Antagonist activity at human CRF1 receptor
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Anatgonist activity at CRF1 receptor (unknown origin)
Binding affinity to CRF1 receptor (unknown origin)
Displacement of [125I]sauvagine from recombinant human CRF1 receptor at 10 uM after 120 mins by scintillation counting analysis relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
In Vitro Inhibition Assay from US Patent US8614213: "Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists"
Assay data:82 Active, 78 Activity ≤ 1 µM, 82 Tested
Homogeneous Time-Resolved Fluorescence Assay from US Patent US8835444: "Cyclohexyl amide derivatives as CRF receptor antagonists"
Assay data:28 Active, 27 Activity ≤ 1 µM, 28 Tested
Binding Assay from US Patent US8530504: "Pyrazolothiazole compound"
Assay data:82 Active, 82 Activity ≤ 1 µM, 82 Tested
Corticotropin Releasing Factor CRF1 Eurofins-Panlabs radioligand binding assay
Assay data:2 Tested
SummaryRelated BioAssays by Target
PRESTO-Tango GPCRome screening (CRHR1)
CRF1/H Cerep selectivity data (BI)
Binding affinity to CRF1(unknown origin) 10 umol/L by radioligand binding assay
Displacement of [125I](Tyr0)-CRF from recombinant full length human recombinant CRF1 expressed in CHO-K1 cells at 10 uM measured after 60 mins by radiometric scintillation analysis relative to control
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
Assay data:20 Active, 17 Activity ≤ 1 µM, 20 Tested
Activity at human CRF1 receptor at 10 uM
Antagonist activity at human CRFR1 expressed in HEK293 cells assessed as inhibition of sauvagine-induced cAMP accumulation by measuring sauvagine EC50 at 1 uM after 30 mins (Rvb = 0.203 nM)
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Ratio of IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes with compound washout to IC50 for displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes without compound washout
Assay data:3 Tested
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