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Assay Detail

CHEMBL1177258

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

Functional
Agonist activity at human PPARgamma-LBD expressed in COS7 cells co-transfected with Gal4 by luciferase based transactivation assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
Hieke M, Ness J, Steri R, Dittrich M, Greiner C, Werz O, Baumann K, Schubert-Zsilavecz M, Weggen S, Zettl H.
J Med Chem (2010) 53 : 4691 -4700
PubMed 20503989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.10 5.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518507 1 5.43
CHEMBL1172001 1 5.37
CHEMBL1173499 1 5.21
CHEMBL1171834 1 5.18
CHEMBL1171831 1 5.16
CHEMBL1173376 1 5.12
CHEMBL461883 1 5.08
CHEMBL1172003 1 5.06
CHEMBL1172019 1 5.05
CHEMBL1172016 1 5.00
CHEMBL1170852 1 4.99
CHEMBL1170076 1 4.98
CHEMBL1170264 1 4.96
CHEMBL1172002 1 4.96
CHEMBL1172000 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518507 EC50 = 3700.0 nM 5.43
CHEMBL1172001 EC50 = 4300.0 nM 5.37
CHEMBL1173499 EC50 = 6100.0 nM 5.21
CHEMBL1171834 EC50 = 6600.0 nM 5.18
CHEMBL1171831 EC50 = 7000.0 nM 5.16
CHEMBL1173376 EC50 = 7500.0 nM 5.12
CHEMBL461883 EC50 = 8300.0 nM 5.08
CHEMBL1172003 EC50 = 8800.0 nM 5.06
CHEMBL1172019 EC50 = 8900.0 nM 5.05
CHEMBL1172016 EC50 = 10000.0 nM 5.00
CHEMBL1170852 EC50 = 10300.0 nM 4.99
CHEMBL1170076 EC50 = 10400.0 nM 4.98
CHEMBL1170264 EC50 = 11000.0 nM 4.96
CHEMBL1172002 EC50 = 11000.0 nM 4.96
CHEMBL1172000 EC50 = 12100.0 nM 4.92