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Assay Detail

CHEMBL2037946

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Functional
Agonist activity at rat GPR109a
7
Total Activities
7
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 SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
Palani A, Rao AU, Chen X, Huang X, Su J, Tang H, Huang Y, Qin J, Xiao D, Degrado S, Sofolarides M, Zhu X, Liu Z, McKittrick B, Zhou W, Aslanian R, Greenlee WJ, Senior M, Cheewatrakoolpong B, Zhang H, Farley C, Cook J, Kurowski S, Li Q, van Heek M, Wang G, Hsieh Y, Li F, Greenfeder S, Chintala M.
ACS Med Chem Lett (2012) 3 : 63 -68
PubMed 24900372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.24 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2036951 1 8.70
CHEMBL2036955 1 8.70
CHEMBL2036948 1 8.40
CHEMBL2036954 1 8.30
CHEMBL2036813 1 8.10
CHEMBL2036958 SCH-900271 2.0 1 8.10
CHEMBL573 NIACIN 4.0 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2036951 EC50 = 2.0 nM 8.70
CHEMBL2036955 EC50 = 2.0 nM 8.70
CHEMBL2036948 EC50 = 4.0 nM 8.40
CHEMBL2036954 EC50 = 5.0 nM 8.30
CHEMBL2036813 EC50 = 8.0 nM 8.10
CHEMBL2036958 SCH-900271 EC50 = 8.0 nM 8.10
CHEMBL573 NIACIN EC50 = 39.0 nM 7.41