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Assay Detail

CHEMBL3399107

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

Binding
Agonist activity at GAL4 tagged human PPARgamma ligand binding domain expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL ↗
48
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.
Zhang H, Ding CZ, Lai Z, Chen SS, Devasthale P, Herpin T, Morton G, Qu F, Ryono D, Smirk R, Wang W, Wu S, Ye XX, Li YX, Apedo A, Farrelly D, Wang T, Gu L, Morgan N, Flynn N, Chu C, Kunselman L, Lippy J, Locke K, O'Malley K, Harrity T, Cap M, Zhang L, Hosagrahara V, Kadiyala P, Xu C, Doweyko AM, Zahler R, Hariharan N, Cheng PT.
Bioorg Med Chem Lett (2015) 25 : 1196 -1205
PubMed 25686852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 6.13 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398436 — — 2 8.05
CHEMBL3398429 — — 1 8.00
CHEMBL3398430 — — 1 7.70
CHEMBL255930 — — 2 7.52
CHEMBL3398443 — — 2 7.52
CHEMBL186179 MURAGLITAZAR 3.0 1 7.46
CHEMBL3398423 — — 1 7.30
CHEMBL3398459 — — 1 6.80
CHEMBL3398442 — — 1 6.52
CHEMBL3398458 — — 1 6.27
CHEMBL3398456 — — 1 6.20
CHEMBL3398449 — — 1 6.20
CHEMBL3398455 — — 1 6.15
CHEMBL3398448 — — 1 5.97
CHEMBL3398457 — — 1 5.93
CHEMBL3398438 — — 2 5.90
CHEMBL3398453 — — 1 5.68
CHEMBL3398446 — — 1 5.60
CHEMBL3398440 — — 1 5.54
CHEMBL3398444 — — 2 5.47
CHEMBL3398435 — — 1 5.38
CHEMBL3398427 — — 1 5.38
CHEMBL3398431 — — 1 5.32
CHEMBL3398425 — — 1 5.25
CHEMBL3398441 — — 1 5.21
CHEMBL3398432 — — 1 5.01
CHEMBL3398439 — — 1 4.88
CHEMBL3398433 — — 1 4.84
CHEMBL3398424 — — 1 4.62
CHEMBL3398464 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398436 — EC50 = 9.0 nM 8.05
CHEMBL3398429 — EC50 = 10.0 nM 8.00
CHEMBL3398430 — EC50 = 20.0 nM 7.70
CHEMBL3398443 — EC50 = 30.0 nM 7.52
CHEMBL255930 — EC50 = 30.0 nM 7.52
CHEMBL186179 MURAGLITAZAR EC50 = 35.0 nM 7.46
CHEMBL3398423 — EC50 = 50.0 nM 7.30
CHEMBL255930 — EC50 = 50.0 nM 7.30
CHEMBL3398459 — EC50 = 160.0 nM 6.80
CHEMBL3398442 — EC50 = 300.0 nM 6.52
CHEMBL3398458 — EC50 = 540.0 nM 6.27
CHEMBL3398456 — EC50 = 630.0 nM 6.20
CHEMBL3398449 — EC50 = 630.0 nM 6.20
CHEMBL3398443 — EC50 = 640.0 nM 6.19
CHEMBL3398455 — EC50 = 710.0 nM 6.15
CHEMBL3398436 — EC50 = 750.0 nM 6.12
CHEMBL3398448 — EC50 = 1060.0 nM 5.97
CHEMBL3398457 — EC50 = 1170.0 nM 5.93
CHEMBL3398438 — EC50 = 1250.0 nM 5.90
CHEMBL3398438 — EC50 = 2000.0 nM 5.70
CHEMBL3398453 — EC50 = 2080.0 nM 5.68
CHEMBL3398446 — EC50 = 2500.0 nM 5.60
CHEMBL3398440 — EC50 = 2850.0 nM 5.54
CHEMBL3398444 — EC50 = 3410.0 nM 5.47
CHEMBL3398444 — EC50 = 3440.0 nM 5.46
CHEMBL3398435 — EC50 = 4180.0 nM 5.38
CHEMBL3398427 — EC50 = 4180.0 nM 5.38
CHEMBL3398431 — EC50 = 4800.0 nM 5.32
CHEMBL3398425 — EC50 = 5650.0 nM 5.25
CHEMBL3398441 — EC50 = 6170.0 nM 5.21
CHEMBL3398432 — EC50 = 9680.0 nM 5.01
CHEMBL3398439 — EC50 = 13300.0 nM 4.88
CHEMBL3398433 — EC50 = 14600.0 nM 4.84
CHEMBL3398424 — EC50 = 24000.0 nM 4.62
CHEMBL3398447 — EC50 > 10000.0 nM -
CHEMBL3398426 — EC50 > 32000.0 nM -
CHEMBL3398450 — EC50 > 10000.0 nM -
CHEMBL3398451 — EC50 > 30000.0 nM -
CHEMBL3398452 — EC50 > 30000.0 nM -
CHEMBL3398437 — EC50 > 10000.0 nM -
CHEMBL3398428 — EC50 > 32000.0 nM -
CHEMBL3398445 — EC50 > 10000.0 nM -
CHEMBL3398460 — EC50 > 10000.0 nM -
CHEMBL3398461 — EC50 > 10000.0 nM -
CHEMBL3398462 — EC50 > 10000.0 nM -
CHEMBL3398463 — EC50 > 10000.0 nM -
CHEMBL3398464 — EC50 > 10000.0 nM -
CHEMBL3398454 — EC50 > 30000.0 nM -