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Assay Detail

CHEMBL3888500

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

Binding
Kinase Activity Assay: After 24 h treatment with the medicament, the cells were lysed with a lysis solution (Cell Culture Lysis buffer, Promega) and centrifuged, and the supernatant was collected. The supernatant was reacted with a fluorescence assay kit (Promega) and counted by a fluorometer (Ascent Fluoroskan FL reader, Thermo Labsystems, Finland), and the relative intensity of luciferase was determined. For the assay of the β-galactosidase activity used in the experiment as the internal reference (the internal reference for calibrating the transfection efficiency), 50 μl of the supernatant was transferred into a fresh microplate, treated with a Promega kit, and the value was read with a microplate reader at a wavelength of 405 nm (Bio-tech Instruments Inc., Winooski, Vt., USA) (Sauerberg, P.; Olsen, G. S.; Jeppesen, L.; Mogensen, J. P. et al., J. Med. Chem., 2007, 50, 1495-1503).
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Compounds having activating effect on subtypes of peroxisome proliferator-activated receptors and its preparation method and uses
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 9.00
CHEMBL3932461 1 8.40
CHEMBL3920204 1 8.30
CHEMBL3972176 1 7.89
CHEMBL3976442 1 7.66
CHEMBL3905699 1 7.60
CHEMBL3914680 1 7.33
CHEMBL3892207 1 7.05
CHEMBL3946222 1 6.16
CHEMBL3904658 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 1.0 nM 9.00
CHEMBL3932461 EC50 = 4.0 nM 8.40
CHEMBL3920204 EC50 = 5.0 nM 8.30
CHEMBL3972176 EC50 = 13.0 nM 7.89
CHEMBL3976442 EC50 = 22.0 nM 7.66
CHEMBL3905699 EC50 = 25.0 nM 7.60
CHEMBL3914680 EC50 = 47.0 nM 7.33
CHEMBL3892207 EC50 = 89.0 nM 7.05
CHEMBL3946222 EC50 = 692.0 nM 6.16
CHEMBL3904658 EC50 = 6761.0 nM 5.17