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Assay Detail

CHEMBL1114855

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

Binding
Agonist activity at human PPARgamma ligand binding domain expressed in human 293T cells co-transfected with Gal4-DBD by luciferase transactivation assay
128
Total Activities
128
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists.
Epple R, Cow C, Xie Y, Azimioara M, Russo R, Wang X, Wityak J, Karanewsky DS, Tuntland T, Nguyêñ-Trân VT, Cuc Ngo C, Huang D, Saez E, Spalding T, Gerken A, Iskandar M, Seidel HM, Tian SS.
J Med Chem (2010) 53 : 77 -105
PubMed 19928766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 128 5.63 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279053 L-165461 1 7.00
CHEMBL1075732 1 6.22
CHEMBL1080365 1 6.01
CHEMBL1075895 1 5.99
CHEMBL1075723 1 5.92
CHEMBL1079669 1 5.88
CHEMBL1075724 1 5.81
CHEMBL1080361 1 5.64
CHEMBL1075894 1 5.60
CHEMBL1079961 1 5.59
CHEMBL1079962 1 5.34
CHEMBL1081950 1 5.25
CHEMBL1080140 1 5.23
CHEMBL1081003 1 5.20
CHEMBL1081786 1 5.16
CHEMBL1080699 1 4.16
CHEMBL1081756 1 -
CHEMBL1079488 1 -
CHEMBL1075772 1 -
CHEMBL1079489 1 -
CHEMBL1081424 1 -
CHEMBL1081591 1 -
CHEMBL1079503 1 -
CHEMBL1079504 1 -
CHEMBL1081602 1 -
CHEMBL1075856 1 -
CHEMBL1081603 1 -
CHEMBL1081949 1 -
CHEMBL1082116 1 -
CHEMBL1080025 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279053 L-165461 EC50 = 100.0 nM 7.00
CHEMBL1075732 EC50 = 600.0 nM 6.22
CHEMBL1080365 EC50 = 980.0 nM 6.01
CHEMBL1075895 EC50 = 1030.0 nM 5.99
CHEMBL1075723 EC50 = 1200.0 nM 5.92
CHEMBL1079669 EC50 = 1310.0 nM 5.88
CHEMBL1075724 EC50 = 1560.0 nM 5.81
CHEMBL1080361 EC50 = 2300.0 nM 5.64
CHEMBL1075894 EC50 = 2490.0 nM 5.60
CHEMBL1079961 EC50 = 2560.0 nM 5.59
CHEMBL1079962 EC50 = 4610.0 nM 5.34
CHEMBL1081950 EC50 = 5660.0 nM 5.25
CHEMBL1080140 EC50 = 5870.0 nM 5.23
CHEMBL1081003 EC50 = 6360.0 nM 5.20
CHEMBL1081786 EC50 = 6890.0 nM 5.16
CHEMBL1080699 EC50 = 70000.0 nM 4.16
CHEMBL1080366 EC50 > 10000.0 nM -
CHEMBL1079981 EC50 > 10000.0 nM -
CHEMBL1079982 EC50 > 10000.0 nM -
CHEMBL1081410 EC50 > 10000.0 nM -
CHEMBL1081045 EC50 > 10000.0 nM -
CHEMBL1080187 EC50 > 10000.0 nM -
CHEMBL1081964 EC50 > 10000.0 nM -
CHEMBL1082131 EC50 > 10000.0 nM -
CHEMBL1080363 EC50 > 10000.0 nM -
CHEMBL1080534 EC50 > 10000.0 nM -
CHEMBL1080312 EC50 > 10000.0 nM -
CHEMBL1081044 EC50 > 10000.0 nM -
CHEMBL1081917 EC50 - -
CHEMBL1075665 EC50 > 10000.0 nM -
CHEMBL210469 EC50 > 10000.0 nM -
CHEMBL1081963 EC50 > 10000.0 nM -
CHEMBL1081951 EC50 > 10000.0 nM -
CHEMBL1079984 EC50 > 10000.0 nM -
CHEMBL1080873 EC50 > 10000.0 nM -
CHEMBL1075705 EC50 > 10000.0 nM -
CHEMBL1081223 EC50 > 10000.0 nM -
CHEMBL1081224 EC50 > 10000.0 nM -
CHEMBL1075725 EC50 > 10000.0 nM -
CHEMBL1081391 EC50 > 10000.0 nM -
CHEMBL1079821 EC50 > 10000.0 nM -
CHEMBL1079983 EC50 > 10000.0 nM -
CHEMBL1080184 EC50 > 10000.0 nM -
CHEMBL1079505 EC50 > 10000.0 nM -
CHEMBL1080172 EC50 > 10000.0 nM -
CHEMBL1075835 EC50 > 10000.0 nM -
CHEMBL1075836 EC50 > 10000.0 nM -
CHEMBL1080173 EC50 > 10000.0 nM -
CHEMBL1082117 EC50 > 10000.0 nM -
CHEMBL1082118 EC50 > 10000.0 nM -