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Assay Detail

CHEMBL983496

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-K1 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.
Deng Q, Frie JL, Marley DM, Beresis RT, Ren N, Cai TQ, Taggart AK, Cheng K, Carballo-Jane E, Wang J, Tong X, Waters MG, Tata JR, Colletti SL.
Bioorg Med Chem Lett (2008) 18 : 4963 -4967
PubMed 18760600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.01 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522649 1 7.62
CHEMBL491002 1 7.47
CHEMBL491003 1 7.26
CHEMBL492220 1 7.06
CHEMBL573 NIACIN 4.0 1 6.89
CHEMBL235740 1 6.85
CHEMBL443733 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522649 IC50 = 24.0 nM 7.62
CHEMBL491002 IC50 = 34.0 nM 7.47
CHEMBL491003 IC50 = 55.0 nM 7.26
CHEMBL492220 IC50 = 87.0 nM 7.06
CHEMBL573 NIACIN IC50 = 130.0 nM 6.89
CHEMBL235740 IC50 = 140.0 nM 6.85
CHEMBL443733 IC50 = 1200.0 nM 5.92