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Assay Detail

CHEMBL942382

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

Binding
Displacement of [3H]rosiglitazone from histidine-tagged PPARgamma ligand binding domain by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands.
Pochetti G, Godio C, Mitro N, Caruso D, Galmozzi A, Scurati S, Loiodice F, Fracchiolla G, Tortorella P, Laghezza A, Lavecchia A, Novellino E, Mazza F, Crestani M.
J Biol Chem (2007) 282 : 17314 -17324
PubMed 17403688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.73 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 7.13
CHEMBL479207 1 7.06
CHEMBL477119 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE Ki = 74.0 nM 7.13
CHEMBL479207 Ki = 88.0 nM 7.06
CHEMBL477119 Ki = 971.0 nM 6.01