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Assay Detail

CHEMBL1119082

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

Binding
Displacement of [3H]niacin from human niacin receptor expressed in CHO-KI cells
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-KI
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Anthranilic acid replacements in a niacin receptor agonist.
Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S.
Bioorg Med Chem Lett (2010) 20 : 3426 -3430
PubMed 20444602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.71 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083138 1 8.52
CHEMBL1084576 1 8.40
CHEMBL1087302 1 8.40
CHEMBL1086354 1 8.22
CHEMBL1084799 1 8.22
CHEMBL1084030 1 8.15
CHEMBL1085414 1 8.13
CHEMBL482698 1 8.10
CHEMBL1086353 1 8.10
CHEMBL1086225 1 8.10
CHEMBL1085655 1 8.07
CHEMBL1084031 1 8.05
CHEMBL1083442 1 8.05
CHEMBL1085653 1 7.96
CHEMBL1085589 1 7.92
CHEMBL1086029 1 7.85
CHEMBL1082294 1 7.82
CHEMBL1083450 1 7.80
CHEMBL1083451 1 7.75
CHEMBL1084841 1 7.72
CHEMBL1083743 1 7.55
CHEMBL1085816 1 7.50
CHEMBL1086355 1 7.47
CHEMBL1085815 1 7.46
CHEMBL1086031 1 7.44
CHEMBL1083174 1 7.37
CHEMBL1083139 1 7.28
CHEMBL1084839 1 7.24
CHEMBL1084840 1 7.07
CHEMBL1086030 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083138 IC50 = 3.0 nM 8.52
CHEMBL1084576 IC50 = 4.0 nM 8.40
CHEMBL1087302 IC50 = 4.0 nM 8.40
CHEMBL1086354 IC50 = 6.0 nM 8.22
CHEMBL1084799 IC50 = 6.0 nM 8.22
CHEMBL1084030 IC50 = 7.0 nM 8.15
CHEMBL1085414 IC50 = 7.4 nM 8.13
CHEMBL482698 IC50 = 8.0 nM 8.10
CHEMBL1086353 IC50 = 8.0 nM 8.10
CHEMBL1086225 IC50 = 8.0 nM 8.10
CHEMBL1085655 IC50 = 8.6 nM 8.07
CHEMBL1084031 IC50 = 9.0 nM 8.05
CHEMBL1083442 IC50 = 9.0 nM 8.05
CHEMBL1085653 IC50 = 11.0 nM 7.96
CHEMBL1085589 IC50 = 12.0 nM 7.92
CHEMBL1086029 IC50 = 14.0 nM 7.85
CHEMBL1082294 IC50 = 15.0 nM 7.82
CHEMBL1083450 IC50 = 16.0 nM 7.80
CHEMBL1083451 IC50 = 18.0 nM 7.75
CHEMBL1084841 IC50 = 19.0 nM 7.72
CHEMBL1083743 IC50 = 28.0 nM 7.55
CHEMBL1085816 IC50 = 32.0 nM 7.50
CHEMBL1086355 IC50 = 34.0 nM 7.47
CHEMBL1085815 IC50 = 35.0 nM 7.46
CHEMBL1086031 IC50 = 36.0 nM 7.44
CHEMBL1083174 IC50 = 43.0 nM 7.37
CHEMBL1083139 IC50 = 52.0 nM 7.28
CHEMBL1084839 IC50 = 57.0 nM 7.24
CHEMBL1084840 IC50 = 85.0 nM 7.07
CHEMBL1086030 IC50 = 120.0 nM 6.92
CHEMBL573 NIACIN IC50 = 140.0 nM 6.85
CHEMBL1084798 IC50 = 280.0 nM 6.55
CHEMBL1086356 IC50 = 420.0 nM 6.38