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Assay Detail

CHEMBL764404

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

Functional
Transcriptional activation of peroxisome proliferator activated receptor gamma
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct 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
EC50 15 6.20 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320553 1 7.36
CHEMBL121 ROSIGLITAZONE 4.0 1 7.05
CHEMBL331798 1 6.51
CHEMBL116043 1 6.47
CHEMBL408 TROGLITAZONE 4.0 1 6.27
CHEMBL595 PIOGLITAZONE 4.0 1 6.23
CHEMBL326947 1 5.52
CHEMBL111841 1 5.25
CHEMBL268513 1 5.15
CHEMBL115448 1 -
CHEMBL115310 1 -
CHEMBL113006 1 -
CHEMBL420314 1 -
CHEMBL113587 1 -
CHEMBL275682 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320553 EC50 = 43.65 nM 7.36
CHEMBL121 ROSIGLITAZONE EC50 = 89.13 nM 7.05
CHEMBL331798 EC50 = 309.03 nM 6.51
CHEMBL116043 EC50 = 338.84 nM 6.47
CHEMBL408 TROGLITAZONE EC50 = 537.03 nM 6.27
CHEMBL595 PIOGLITAZONE EC50 = 588.84 nM 6.23
CHEMBL326947 EC50 = 3019.95 nM 5.52
CHEMBL111841 EC50 = 5623.41 nM 5.25
CHEMBL268513 EC50 = 7079.46 nM 5.15
CHEMBL115448 EC50 < 10000.0 nM -
CHEMBL115310 EC50 < 10000.0 nM -
CHEMBL113006 EC50 < 10000.0 nM -
CHEMBL420314 EC50 < 10000.0 nM -
CHEMBL113587 EC50 < 10000.0 nM -
CHEMBL275682 EC50 < 10000.0 nM -