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Assay Detail

CHEMBL983499

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Functional
Agonist activity at human GPR109A receptor expressed in CHO-K1 cells by [35S]GTPgammaS guanine nucleotide exchange assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 7 5.91 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522649 1 6.42
CHEMBL491002 1 6.27
CHEMBL491003 1 6.03
CHEMBL235740 1 6.00
CHEMBL443733 1 5.92
CHEMBL573 NIACIN 4.0 1 5.85
CHEMBL228244 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522649 EC50 = 380.0 nM 6.42
CHEMBL491002 EC50 = 540.0 nM 6.27
CHEMBL491003 EC50 = 940.0 nM 6.03
CHEMBL235740 EC50 = 1000.0 nM 6.00
CHEMBL443733 EC50 = 1200.0 nM 5.92
CHEMBL573 NIACIN EC50 = 1400.0 nM 5.85
CHEMBL228244 EC50 = 12500.0 nM 4.90