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Assay Detail

CHEMBL901267

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Functional
Agonist activity at mouse GPR109A by [35S]GTP-gamma-S binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL4420)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.
Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
J Med Chem (2007) 50 : 6303 -6306
PubMed 17994679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.19 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573 NIACIN 4.0 1 6.57
CHEMBL391813 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573 NIACIN EC50 = 270.0 nM 6.57
CHEMBL391813 EC50 = 1600.0 nM 5.80