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Assay Detail

CHEMBL971505

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

Binding
Displacement of [3H]nicotinic acid from mouse GPR109a receptor
26
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.
Imbriglio JE, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, Tria S, Schrader TO, Jung JK, Esser C, Taggart AK, Cheng K, Carballo-Jane E, Gerard Waters M, Tata JR, Colletti SL.
Bioorg Med Chem Lett (2009) 19 : 2121 -2124
PubMed 19307116 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.24 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520137 2 7.40
CHEMBL509541 2 7.22
CHEMBL507182 1 7.16
CHEMBL519966 1 7.10
CHEMBL520676 1 7.05
CHEMBL573 NIACIN 4.0 1 6.85
CHEMBL502716 1 6.85
CHEMBL500239 1 6.58
CHEMBL520675 1 6.51
CHEMBL504980 1 6.47
CHEMBL519811 1 6.28
CHEMBL484172 1 6.10
CHEMBL483142 1 6.07
CHEMBL456145 1 5.92
CHEMBL519338 1 5.89
CHEMBL483141 1 5.80
CHEMBL482943 1 5.77
CHEMBL501585 1 5.60
CHEMBL447050 1 5.51
CHEMBL482979 1 5.44
CHEMBL485195 1 5.40
CHEMBL485194 1 5.38
CHEMBL520159 1 5.05
CHEMBL519689 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520137 IC50 = 40.0 nM 7.40
CHEMBL509541 IC50 = 60.0 nM 7.22
CHEMBL507182 IC50 = 70.0 nM 7.16
CHEMBL520137 IC50 = 70.0 nM 7.16
CHEMBL519966 IC50 = 80.0 nM 7.10
CHEMBL520676 IC50 = 90.0 nM 7.05
CHEMBL573 NIACIN IC50 = 140.0 nM 6.85
CHEMBL502716 IC50 = 140.0 nM 6.85
CHEMBL509541 IC50 = 210.0 nM 6.68
CHEMBL500239 IC50 = 260.0 nM 6.58
CHEMBL520675 IC50 = 310.0 nM 6.51
CHEMBL504980 IC50 = 340.0 nM 6.47
CHEMBL519811 IC50 = 520.0 nM 6.28
CHEMBL484172 IC50 = 800.0 nM 6.10
CHEMBL483142 IC50 = 850.0 nM 6.07
CHEMBL456145 IC50 = 1200.0 nM 5.92
CHEMBL519338 IC50 = 1300.0 nM 5.89
CHEMBL483141 IC50 = 1600.0 nM 5.80
CHEMBL482943 IC50 = 1700.0 nM 5.77
CHEMBL501585 IC50 = 2500.0 nM 5.60
CHEMBL447050 IC50 = 3100.0 nM 5.51
CHEMBL482979 IC50 = 3600.0 nM 5.44
CHEMBL485195 IC50 = 4000.0 nM 5.40
CHEMBL485194 IC50 = 4200.0 nM 5.38
CHEMBL520159 IC50 = 9000.0 nM 5.05
CHEMBL519689 IC50 = 11000.0 nM 4.96