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Assay Detail

CHEMBL971520

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

Functional
Inhibition of lipolysis in IBMX-stimulated human adipocytes assessed as glycerol release after 5 hrs
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Adipocyte
Confidence 1 — Organism
Curated By Autocuration

Target

Adipocyte (CHEMBL614658)
Type CELL-LINE

Publication

Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.
J Med Chem (2009) 52 : 2587 -2602
PubMed 19309152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521326 1 7.70
CHEMBL483352 1 7.22
CHEMBL483337 1 7.22
CHEMBL573 NIACIN 4.0 1 7.16
CHEMBL482768 1 6.96
CHEMBL520299 1 6.82
CHEMBL484783 1 6.70
CHEMBL520136 1 6.55
CHEMBL520513 1 5.58
CHEMBL482963 1 -
CHEMBL483160 1 -
CHEMBL483353 1 -
CHEMBL484604 1 -
CHEMBL484605 1 -
CHEMBL520620 1 -
CHEMBL482980 1 -
CHEMBL483996 1 -
CHEMBL485184 1 -
CHEMBL485185 1 -
CHEMBL522649 1 -
CHEMBL485196 1 -
CHEMBL483139 1 -
CHEMBL483140 1 -
CHEMBL483336 1 -
CHEMBL485326 1 -
CHEMBL485327 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521326 IC50 = 20.0 nM 7.70
CHEMBL483352 IC50 = 60.0 nM 7.22
CHEMBL483337 IC50 = 60.0 nM 7.22
CHEMBL573 NIACIN IC50 = 70.0 nM 7.16
CHEMBL482768 IC50 = 110.0 nM 6.96
CHEMBL520299 IC50 = 150.0 nM 6.82
CHEMBL484783 IC50 = 200.0 nM 6.70
CHEMBL520136 IC50 = 280.0 nM 6.55
CHEMBL520513 IC50 = 2600.0 nM 5.58
CHEMBL482963 IC50 - -
CHEMBL483160 IC50 - -
CHEMBL483353 IC50 - -
CHEMBL484604 IC50 - -
CHEMBL484605 IC50 - -
CHEMBL520620 IC50 - -
CHEMBL482980 IC50 - -
CHEMBL483996 IC50 - -
CHEMBL485184 IC50 - -
CHEMBL485185 IC50 - -
CHEMBL522649 IC50 - -
CHEMBL485196 IC50 - -
CHEMBL483139 IC50 - -
CHEMBL483140 IC50 - -
CHEMBL483336 IC50 - -
CHEMBL485326 IC50 - -
CHEMBL485327 IC50 - -