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Assay Detail

CHEMBL762149

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

Binding
Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma)
15
Total Activities
15
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

Synthesis and biological activity of a novel series of indole-derived PPARgamma agonists.
Henke BR, Adkison KK, Blanchard SG, Leesnitzer LM, Mook RA, Plunket KD, Ray JA, Roberson C, Unwalla R, Willson TM.
Bioorg Med Chem Lett (1999) 9 : 3329 -3334
PubMed 10612594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.17 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 7.33
CHEMBL320553 1 7.32
CHEMBL331798 1 6.83
CHEMBL275682 1 6.67
CHEMBL408 TROGLITAZONE 4.0 1 6.52
CHEMBL116043 1 6.31
CHEMBL111841 1 6.26
CHEMBL595 PIOGLITAZONE 4.0 1 5.91
CHEMBL115448 1 5.72
CHEMBL420314 1 5.43
CHEMBL268513 1 5.41
CHEMBL115137 1 5.35
CHEMBL326947 1 5.14
CHEMBL115310 1 -
CHEMBL113587 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE Ki = 46.77 nM 7.33
CHEMBL320553 Ki = 47.86 nM 7.32
CHEMBL331798 Ki = 147.91 nM 6.83
CHEMBL275682 Ki = 213.8 nM 6.67
CHEMBL408 TROGLITAZONE Ki = 302.0 nM 6.52
CHEMBL116043 Ki = 489.78 nM 6.31
CHEMBL111841 Ki = 549.54 nM 6.26
CHEMBL595 PIOGLITAZONE Ki = 1230.27 nM 5.91
CHEMBL115448 Ki = 1905.46 nM 5.72
CHEMBL420314 Ki = 3715.35 nM 5.43
CHEMBL268513 Ki = 3890.45 nM 5.41
CHEMBL115137 Ki = 4466.84 nM 5.35
CHEMBL326947 Ki = 7244.36 nM 5.14
CHEMBL115310 Ki < 10000.0 nM -
CHEMBL113587 Ki < 10000.0 nM -