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Assay Detail

CHEMBL4008127

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

Binding
Binding affinity to PPARgamma (unknown origin) assessed as thermodynamic dissociation constant by SPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
Piemontese L, Cerchia C, Laghezza A, Ziccardi P, Sblano S, Tortorella P, Iacobazzi V, Infantino V, Convertini P, Dal Piaz F, Lupo A, Colantuoni V, Lavecchia A, Loiodice F.
Eur J Med Chem (2017) 127 : 379 -397
PubMed 28076827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.89 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 8.92
CHEMBL4073499 1 8.43
CHEMBL4092600 1 8.31
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.89
CHEMBL153057 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE Kd = 1.2 nM 8.92
CHEMBL4073499 Kd = 3.7 nM 8.43
CHEMBL4092600 Kd = 4.9 nM 8.31
CHEMBL295416 PIRINIXIC ACID Kd = 1297.3 nM 5.89
CHEMBL153057 Kd - -