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Assay Detail

CHEMBL1119865

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

Functional
Antidyslipidemic activity in human adipocytes assessed as inhibition of isoproteranol-induced production of free fatty acids
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Adipocyte
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).
Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG.
Bioorg Med Chem Lett (2010) 20 : 2797 -2800
PubMed 20363624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.78 7.22
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573 NIACIN 4.0 1 7.22
CHEMBL1085289 3-(1H-TETRAZOL-5-YL)-4,4A,5,5A-TETRAHYDRO-1H-CYCLOPROPA[4,5]CYCLOPENTA[1,2-C]PYRAZOLE (STRUCTURAL MIX) 2 7.05
CHEMBL456145 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573 NIACIN IC50 = 60.0 nM 7.22
CHEMBL1085289 3-(1H-TETRAZOL-5-YL)-4,4A,5,5A-TETRAHYDRO-1H-CYCLOPROPA[4,5]CYCLOPENTA[1,2-C]PYRAZOLE (STRUCTURAL MIX) IC50 = 90.0 nM 7.05
CHEMBL456145 IC50 = 870.0 nM 6.06
CHEMBL1085289 3-(1H-TETRAZOL-5-YL)-4,4A,5,5A-TETRAHYDRO-1H-CYCLOPROPA[4,5]CYCLOPENTA[1,2-C]PYRAZOLE (STRUCTURAL MIX) Inhibition - % -