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Assay Detail

CHEMBL1947834

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

Functional
Partial agonist activity at human PPARgamma LBD assessed as activation of PGC1 by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
Liu W, Lau F, Liu K, Wood HB, Zhou G, Chen Y, Li Y, Akiyama TE, Castriota G, Einstein M, Wang C, McCann ME, Doebber TW, Wu M, Chang CH, McNamara L, McKeever B, Mosley RT, Berger JP, Meinke PT.
J Med Chem (2011) 54 : 8541 -8554
PubMed 22070604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.80 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946409 1 9.00
CHEMBL1947143 1 8.70
CHEMBL1947147 1 8.70
CHEMBL107367 FARGLITAZAR 2.0 1 8.40
CHEMBL461571 1 8.30
CHEMBL562864 1 8.30
CHEMBL1947146 1 8.10
CHEMBL1947144 1 7.54
CHEMBL121 ROSIGLITAZONE 4.0 1 6.96
CHEMBL1946568 1 6.34
CHEMBL1946570 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946409 EC50 = 1.0 nM 9.00
CHEMBL1947143 EC50 = 2.0 nM 8.70
CHEMBL1947147 EC50 = 2.0 nM 8.70
CHEMBL107367 FARGLITAZAR EC50 = 4.0 nM 8.40
CHEMBL461571 EC50 = 5.0 nM 8.30
CHEMBL562864 EC50 = 5.0 nM 8.30
CHEMBL1947146 EC50 = 8.0 nM 8.10
CHEMBL1947144 EC50 = 29.0 nM 7.54
CHEMBL121 ROSIGLITAZONE EC50 = 110.0 nM 6.96
CHEMBL1946568 EC50 = 460.0 nM 6.34
CHEMBL1946570 EC50 = 3240.0 nM 5.49