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Assay Detail

CHEMBL1002177

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

Binding
Displacement of [3H]nicotinic acid from human GPR109a receptor expressed in CHO cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL3785)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 2 6.80 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573 NIACIN 4.0 1 7.30
CHEMBL456145 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573 NIACIN Ki = 50.0 nM 7.30
CHEMBL456145 Ki = 505.0 nM 6.30