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Assay Detail

CHEMBL1001830

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Binding
Agonist activity at human niacin receptor expressed in CHO cells by GTPgammaS binding assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Raghavan S, Tria GS, Shen HC, Ding FX, Taggart AK, Ren N, Wilsie LC, Krsmanovic ML, Holt TG, Wolff MS, Waters MG, Hammond ML, Tata JR, Colletti SL.
Bioorg Med Chem Lett (2008) 18 : 3163 -3167
PubMed 18477506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.35 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482480 1 8.22
CHEMBL482481 1 7.75
CHEMBL236163 1 6.96
CHEMBL483934 1 6.46
CHEMBL484718 1 6.42
CHEMBL235741 1 6.23
CHEMBL484719 1 6.16
CHEMBL484717 1 6.08
CHEMBL573 NIACIN 4.0 1 6.00
CHEMBL519178 1 5.94
CHEMBL482514 1 5.92
CHEMBL228244 1 5.22
CHEMBL484122 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482480 IC50 = 6.0 nM 8.22
CHEMBL482481 IC50 = 18.0 nM 7.75
CHEMBL236163 IC50 = 110.0 nM 6.96
CHEMBL483934 IC50 = 350.0 nM 6.46
CHEMBL484718 IC50 = 380.0 nM 6.42
CHEMBL235741 IC50 = 590.0 nM 6.23
CHEMBL484719 IC50 = 690.0 nM 6.16
CHEMBL484717 IC50 = 840.0 nM 6.08
CHEMBL573 NIACIN IC50 = 1000.0 nM 6.00
CHEMBL519178 IC50 = 1160.0 nM 5.94
CHEMBL482514 IC50 = 1210.0 nM 5.92
CHEMBL228244 IC50 = 6000.0 nM 5.22
CHEMBL484122 IC50 = 6300.0 nM 5.20