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Glosensor cAMP assay from US Patent US20240059655: "HETEROCYCLIC G-PROTEIN-COUPLED RECEPTOR 52 (GPR52) AGONISTS"
Assay data:69 Active, 62 Activity ≤ 1 µM, 69 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Agonist activity at human GPR52 expressed in HEK293F assessed as cAMP accumulation preincubated for 30 mins followed by cAMP detection reagent and measured after 1 hr by HTRF analysis
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of GPR52 (unknown origin)
Assay data:3 Active, 2 Activity ≤ 1 µM, 4 Tested
Homogeneous Time-Resolved Fluorescence (HTRF) Assay from US Patent US11780827: "Substituted 3-phenoxyazetidin-1-yl-pyrazines"
Assay data:46 Active, 46 Activity ≤ 1 µM, 46 Tested
Affinity On-target Cellular interaction (Cell-based cAMP assay) EUB0000336a GPR52
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMRelated BioAssays by Target
Affinity On-target Cellular interaction (Cell-based cAMP assay) EUB0000317b GPR52
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Affinity Phenotypic Cellular interaction (Alphascreen (cAMP increase in human GPR52 expressed CHO cell line)) EUB0000317b GPR52
PRESTO-Tango GPCRome screening (GPR52)
Assay data:1 Tested
SummaryRelated BioAssays by Target
PRESTO-Tango GPCRome screening (GPR21)
CHO-based cAMP assay (mouse)
CHO-based cAMP assay (human)
Assay data:1 Active, 2 Activity ≤ 1 µM, 2 Tested
In vivo agonist activity at GPR52 in C57BL/6 mouse assessed as inhibition of basal locomotor activity at 10 mg/kg, po measured for 60 mins starting at 15 mins post-drug challenge
Assay data:13 Tested
In vivo agonist activity at GPR52 in po dosed C57BL/6 mouse assessed as inhibition of basal locomotor activity measured for 60 mins starting at 15 mins post-drug challenge
Agonist activity at GPR52 (unknown origin) expressed in CHO-K1 or HEK293 cells assessed as intracellular cAMP accumulation incubated for 1 hr by HTRF assay
Assay data:208 Active, 207 Activity ≤ 1 µM, 208 Tested
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in aggregation of mHTT levels in cortex at 5 mg/kg, iv
SummaryPubMed CitationRelated BioAssays by Target
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in soluble mHTT levels in cortex at 5 mg/kg, iv
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in aggregation of mHTT levels in striatum at 5 mg/kg, iv
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in soluble mHTT levels in striatum at 5 mg/kg, iv
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in aggregation of mHTT at 0.5 mM, icv
In-vivo antagonist activity at GPR52 in HdhQ140 mouse model with GPR52 knockdown assessed as decrease in soluble mHTT levels at 0.5 mM, icv
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