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Assay Detail

CHEMBL921658

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Functional
Agonist activity at GPR109A receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced intracellular cAMP production by Flashplate assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Nicotinic acid receptor agonists differentially activate downstream effectors.
Richman JG, Kanemitsu-Parks M, Gaidarov I, Cameron JS, Griffin P, Zheng H, Guerra NC, Cham L, Maciejewski-Lenoir D, Behan DP, Boatman D, Chen R, Skinner P, Ornelas P, Waters MG, Wright SD, Semple G, Connolly DT.
J Biol Chem (2007) 282 : 18028 -18036
PubMed 17452318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.41 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393428 1 5.89
CHEMBL255877 1 5.77
CHEMBL429495 1 5.66
CHEMBL238002 1 5.58
CHEMBL394441 1 5.38
CHEMBL573 NIACIN 4.0 1 4.17
CHEMBL391574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393428 IC50 = 1300.0 nM 5.89
CHEMBL255877 IC50 = 1700.0 nM 5.77
CHEMBL429495 IC50 = 2200.0 nM 5.66
CHEMBL238002 IC50 = 2600.0 nM 5.58
CHEMBL394441 IC50 = 4200.0 nM 5.38
CHEMBL573 NIACIN IC50 = 67300.0 nM 4.17
CHEMBL391574 IC50 = 434000.0 nM -