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Assay Detail

CHEMBL1002180

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity against mouse GPR109a assessed as GTPgammaS binding
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL4420)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.
Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG.
J Med Chem (2008) 51 : 5101 -5108
PubMed 18665582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.40 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL456145 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL456145 EC50 = 400.0 nM 6.40