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Assay Detail

CHEMBL762737

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

Binding
In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
Mogensen JP, Jeppesen L, Bury PS, Pettersson I, Fleckner J, Nehlin J, Frederiksen KS, Albrektsen T, Din N, Mortensen SB, Svensson LA, Wassermann K, Wulff EM, Ynddal L, Sauerberg P.
Bioorg Med Chem Lett (2003) 13 : 257 -260
PubMed 12482434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.89 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 6.80
CHEMBL86658 1 6.77
CHEMBL328455 1 6.52
CHEMBL672 FENOFIBRATE 4.0 1 6.24
CHEMBL24038 RAGAGLITAZAR 2.0 1 6.24
CHEMBL420973 1 6.22
CHEMBL87928 1 6.10
CHEMBL87307 1 6.05
CHEMBL89152 1 5.82
CHEMBL421729 1 5.77
CHEMBL89996 1 5.70
CHEMBL328099 1 5.66
CHEMBL314483 1 5.57
CHEMBL86817 1 5.54
CHEMBL87380 1 5.51
CHEMBL86657 1 5.48
CHEMBL315048 1 5.40
CHEMBL86688 1 5.37
CHEMBL327481 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 160.0 nM 6.80
CHEMBL86658 EC50 = 170.0 nM 6.77
CHEMBL328455 EC50 = 300.0 nM 6.52
CHEMBL672 FENOFIBRATE EC50 = 570.0 nM 6.24
CHEMBL24038 RAGAGLITAZAR EC50 = 570.0 nM 6.24
CHEMBL420973 EC50 = 600.0 nM 6.22
CHEMBL87928 EC50 = 800.0 nM 6.10
CHEMBL87307 EC50 = 900.0 nM 6.05
CHEMBL89152 EC50 = 1500.0 nM 5.82
CHEMBL421729 EC50 = 1700.0 nM 5.77
CHEMBL89996 EC50 = 2000.0 nM 5.70
CHEMBL328099 EC50 = 2200.0 nM 5.66
CHEMBL314483 EC50 = 2700.0 nM 5.57
CHEMBL86817 EC50 = 2900.0 nM 5.54
CHEMBL87380 EC50 = 3100.0 nM 5.51
CHEMBL86657 EC50 = 3300.0 nM 5.48
CHEMBL315048 EC50 = 4000.0 nM 5.40
CHEMBL86688 EC50 = 4300.0 nM 5.37
CHEMBL327481 EC50 = 8500.0 nM 5.07