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Inhibitory Activity Assay from US Patent US20240158413: "FUSED POLYCYCLIC SUBSTITUTED 5-CARBOXYLIC ACID THIENOPYRIMIDINE DIONE COMPOUND AND USE THEREOF"
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHR
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Receptor Activity Assay from US Patent US10633388: "Pyrazolopyrimidone derivatives and methods of use thereof"
Assay data:14 Active, 11 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
125I-Leuprorelin Binding Assay from US Patent US9346822: "Thienopyrimidine compounds and use thereof"
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
FLIPR Calcium Assay from US Patent US9040693: "Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof"
Assay data:15 Active, 15 Activity ≤ 1 µM, 15 Tested
Activity Assay from US Patent US10344034: "Pyrazolopyrimidone or Pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof"
Assay data:13 Active, 9 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
PRESTO-Tango GPCRome screening (GNRHR)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Mechanistic assay measuring cellular IP1
Binding assay (Tag Lite)
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 4 Tested
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation rate constant by TR-FRET assay
Assay data:4 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as association rate constant by TR-FRET assay
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as residence time by TR-FRET assay
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 5 Tested
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