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Assay Detail

CHEMBL1106879

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

Functional
Agonist activity at rat GPR109A receptor by [35S]GTPgammaS binding assay
5
Total Activities
4
Compounds Tested
2
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 a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.
Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
J Med Chem (2010) 53 : 2666 -2670
PubMed 20184326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 4 - -
EC50 1 5.34 5.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1086657 1 5.34
CHEMBL237248 1 -
CHEMBL1086656 2 -
CHEMBL1087302 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1086657 EC50 = 4600.0 nM 5.34
CHEMBL237248 Activity - -
CHEMBL1086656 Activity - -
CHEMBL1086656 Activity - -
CHEMBL1087302 Activity - -