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Assay Detail

CHEMBL1010538

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Functional
Agonist activity at rat GPR109A expressed by [35S]GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL4731)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
J Med Chem (2009) 52 : 2587 -2602
PubMed 19309152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.87 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573 NIACIN 4.0 1 6.17
CHEMBL482768 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573 NIACIN EC50 = 670.0 nM 6.17
CHEMBL482768 EC50 = 2700.0 nM 5.57