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Allosteric antagonist activity at human TSHR expressed in CHO cells assessed as inhibition of bTSH-induced cAMP production incubated for 2 hrs by luminescence assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human TSHR in HEK293 cells assessed as inhibition of bTSH-induced cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay
Antagonist activity at human TSHR expressed in HEK293 cells assessed as reduction in cAMP production by measuring its efficacy at 10 uM incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay
Assay data:23 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human TSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay
Assay data:23 Active, 23 Activity ≤ 1 µM, 23 Tested
Selectivity interaction (hTSH antagonism experiment) EUB0000240b TSHR
Assay data:1 Tested
SummaryRelated BioAssays by Target
Antagonist Activity Assay from US Patent US9174940: "TSH receptor antagonizing tetrahydroquinoline compounds"
Assay data:24 Active, 24 Activity ≤ 1 µM, 24 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Cell-based assay (TSH Antagonism)
PRESTO-Tango GPCRome screening (TSHR)
Antagonist activity at human thyroid stimulating hormone receptor expressed in rat HTC133 cells assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition and measured after 60 mins by cell based TR-FRET assay
Assay data:1 Active, 5 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
qHTS assay to identify small molecule antagonists of the thyroid stimulating hormone receptor (TSHR) signaling pathway: Summary
Assay data:316 Active, 6 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
qHTS assay to identify small molecule agonists or antagonists of the thyroid stimulating hormone receptor (TSHR) signaling pathway - wild type cell line counter screen: Summary
Assay data:42 Active, 18 Activity ≤ 1 µM, 9667 Tested
qHTS assay to identify small molecule antagonists of the thyroid stimulating hormone receptor (TSHR) signaling pathway
Assay data:205 Active, 1 Activity ≤ 1 nM, 56 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
qHTS assay to identify small molecule agonists of the thyroid stimulating hormone receptor (TSHR) signaling pathway: Summary
Assay data:415 Active, 34 Activity ≤ 1 µM, 9667 Tested
qHTS assay to identify small molecule agonists of the thyroid stimulating hormone receptor (TSHR) signaling pathway
Assay data:320 Active, 42 Activity ≤ 1 µM, 9667 Tested
Agonist activity at TSHR (unknown origin) transiently transfected HEK-EM293 cells assessed as cAMP level after 1 hr by ELISA relative to N-(4-(5-(3-Benzyl-5-hydroxy-4-oxo-1,2,3,4-tetrahydroquinazolin-2-yl)-2-methoxybenzyloxy)phenyl)acetamide
Agonist activity at TSHR (unknown origin) transiently transfected HEK-EM293 cells assessed as cAMP level after 1 hr by ELISA
Assay data:19 Active, 11 Activity ≤ 1 µM, 24 Tested
Agonist activity at TSHR (unknown origin)
Assay data:1 Active, 1 Tested
Antagonists of the Thyroid Stimulating Hormone Receptor: Validation
Assay data:1 Activity ≤ 1 µM, 1280 Tested
SummaryCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
Antagonists of the Thyroid Stimulating Hormone Receptor: Summary
SummaryRelated BioAssays by DepositorRelated BioAssays by Same ProjectRelated BioAssays by Target
qHTS Assay for Antagonists of the Thyroid Stimulating Hormone Receptor: SAR for Probe
Assay data:4 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 119 Tested
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