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Binding affinity towards human CRHR2 in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:284 Tested
SummaryRelated BioAssays by Target
Binding affinity towards human CRHR1 in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:288 Tested
Binding affinity to human CRF1 receptor assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human recombinant CRF1 in HEK cell line incubated for 2 hrs by MicroBeta scintillation counter method
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity to human recombinant CRF2 in HEK cell line assessed as inhibition constant incubated for 4 to 5 hrs by Scintillation Proximity Assay
Assay data:1 Tested
Binding affinity to human recombinant CRF1 in HEK cell line assessed as inhibition constant incubated for 2 hrs by MicroBeta scintillation counter method
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
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
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
In Vitro Binding Autoradiography from Article 10.1021/jm900025h: "Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists."
Assay data:29 Active, 29 Activity ≤ 1 µM, 30 Tested
In Vitro Binding Autoradiography from Article 10.1021/jm9000242: "8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists."
Assay data:44 Active, 2 Activity ≤ 1 nM, 44 Activity ≤ 1 µM, 44 Tested
Receptor Binding Assay from Article 10.1021/jm0611410: "Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling."
Assay data:20 Active, 2 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 20 Tested
Receptor Binding Assay from Article 10.1021/jm070579c: "2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists."
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
Receptor Binding Assay from Article 10.1021/jm070578k: "Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists."
Assay data:31 Active, 30 Activity ≤ 1 µM, 33 Tested
Corticotropin Releasing Factor CRF1 Eurofins-Panlabs radioligand binding assay
Assay data:2 Tested
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