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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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
Rat CRF1 receptor (Corticotropin-releasing factor receptors)
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
Assay data:28 Active, 2 Activity ≤ 1 nM, 28 Activity ≤ 1 µM, 28 Tested
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
Assay data:14 Active, 4 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 15 Tested
Binding affinity to CRFR1 in Sprague-Dawley rat cerebellum at 1.3 nM after 40 mins by autoradiography
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to CRFR1 in Sprague-Dawley rat neocortex at 1.3 nM after 40 mins by autoradiography
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
Assay data:10 Active, 3 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
Antagonist activity at rat CFR1R
Assay data:43 Active, 2 Activity ≤ 1 nM, 42 Activity ≤ 1 µM, 43 Tested
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [125I]CRF from rat CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
Displacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma counting
Antagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
Assay data:7 Active, 7 Activity ≤ 1 µM, 8 Tested
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