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Antagonist activity at human NR13 in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:13 Active, 3 Activity ≤ 1 µM, 36 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity towards human NR1I2 in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:101 Active, 19 Activity ≤ 1 µM, 846 Tested
Antagonist activity at human NR1H3 in an in vitro cell free assay measured by time-resolved fluorescence resonance energy transfer method
Assay data:2 Active, 36 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity towards human EDNRB in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 298 Tested
Binding affinity towards human EDNRA in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 819 Tested
Binding affinity to recombinant human ETA
Assay data:3 Active, 2 Activity ≤ 1 µM, 4 Tested
Nuclear factor erythroid 2-related factor 2/antioxidant responsive element (Nrf2/ARE) small molecule agonists: luciferase reporter gene qHTS assay in human keratinocytes
Assay data:1099 Active, 1 Activity ≤ 1 nM, 143 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same Project
Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: luciferase cell-based qHTS assay
Assay data:2147 Active, 1 Activity ≤ 1 nM, 377 Activity ≤ 1 µM, 5242 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Antagonist activity at ET-B receptor (unknown origin)
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at ET-A receptor (unknown origin)
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Displacement of 125I-ET1 from human placenta ETB receptor
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of 125I-ET1 from human smooth muscle ETA receptor
Antagonist activity at rat aortic ring ETA receptor in presence of ET1
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
Displacement of radioligand from ETB receptor in human placenta cell membranes
Assay data:10 Active, 8 Activity ≤ 1 µM, 10 Tested
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
Assay data:8 Active, 3 Activity ≤ 1 µM, 12 Tested
Antagonist activity at ETB receptor (unknown origin) assessed as effect on G protein-mediated smooth muscle contraction
Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
Assay data:1 Active, 1 Tested
Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as reduction in mean pulmonary artery pressure at 100 mg/kg administered once daily for 21 days starting from 21 days post-MCT challenge by right cardiac catheter method
Assay data:3 Active, 3 Tested
SummaryCompounds, ActivePubMed Citation
Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as reduction in mean pulmonary artery pressure at 25 mg/kg administered once daily for 21 days starting from 21 days post-MCT challenge by right cardiac catheter method
Anti-hypersensitive activity in MCT-induced pulmonary arterial hypertension Sprague-Dawley rat model assessed as reduction in mean pulmonary artery pressure at 1 mg/kg administered once daily for 21 days starting from 21 days post-MCT challenge by right cardiac catheter method
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