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Assay Detail

CHEMBL956508

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

Binding
Displacement of [3H]rosigliatzone from PPARgamma in rat adipocytes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL4797)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New PPARgamma ligands based on 2-hydroxy-1,4-naphthoquinone: computer-aided design, synthesis, and receptor-binding studies.
Sundriyal S, Viswanad B, Bharathy E, Ramarao P, Chakraborti AK, Bharatam PV.
Bioorg Med Chem Lett (2008) 18 : 3192 -3195
PubMed 18482837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.65 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482525 1 6.70
CHEMBL595 PIOGLITAZONE 4.0 1 6.16
CHEMBL519968 1 5.72
CHEMBL482524 1 5.44
CHEMBL482531 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482525 IC50 = 200.0 nM 6.70
CHEMBL595 PIOGLITAZONE IC50 = 700.0 nM 6.16
CHEMBL519968 IC50 = 1900.0 nM 5.72
CHEMBL482524 IC50 = 3600.0 nM 5.44
CHEMBL482531 IC50 = 56200.0 nM 4.25