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Assay Detail

CHEMBL886573

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

Binding
Displacement of fluorescein labeled ligand from PPARgamma receptor by fluorescence polarization assay
24
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
Devasthale PV, Chen S, Jeon Y, Qu F, Ryono DE, Wang W, Zhang H, Cheng L, Farrelly D, Golla R, Grover G, Ma Z, Moore L, Seethala R, Sun W, Doweyko AM, Chandrasena G, Sleph P, Hariharan N, Cheng PT.
Bioorg Med Chem Lett (2007) 17 : 2312 -2316
PubMed 17292606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.33 7.17
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429823 1 7.17
CHEMBL245656 1 6.96
CHEMBL246473 1 6.87
CHEMBL394967 1 6.84
CHEMBL394947 1 6.74
CHEMBL107367 FARGLITAZAR 2.0 1 6.66
CHEMBL247925 1 6.64
CHEMBL246272 1 6.64
CHEMBL246270 1 6.62
CHEMBL121 ROSIGLITAZONE 4.0 1 6.59
CHEMBL397120 1 6.55
CHEMBL394948 1 6.55
CHEMBL395191 1 6.32
CHEMBL396694 1 6.27
CHEMBL248906 1 6.17
CHEMBL247926 1 6.12
CHEMBL428748 1 6.11
CHEMBL396696 1 5.92
CHEMBL371120 1 5.75
CHEMBL248530 1 5.64
CHEMBL245674 1 5.54
CHEMBL247720 1 5.48
CHEMBL394968 1 5.34
CHEMBL247719 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429823 IC50 = 67.0 nM 7.17
CHEMBL245656 IC50 = 110.0 nM 6.96
CHEMBL246473 IC50 = 134.0 nM 6.87
CHEMBL394967 IC50 = 145.0 nM 6.84
CHEMBL394947 IC50 = 183.0 nM 6.74
CHEMBL107367 FARGLITAZAR IC50 = 217.0 nM 6.66
CHEMBL247925 IC50 = 227.0 nM 6.64
CHEMBL246272 IC50 = 230.0 nM 6.64
CHEMBL246270 IC50 = 240.0 nM 6.62
CHEMBL121 ROSIGLITAZONE IC50 = 256.0 nM 6.59
CHEMBL397120 IC50 = 280.0 nM 6.55
CHEMBL394948 IC50 = 284.0 nM 6.55
CHEMBL395191 IC50 = 480.0 nM 6.32
CHEMBL396694 IC50 = 540.0 nM 6.27
CHEMBL248906 IC50 = 670.0 nM 6.17
CHEMBL247926 IC50 = 767.0 nM 6.12
CHEMBL428748 IC50 = 773.0 nM 6.11
CHEMBL396696 IC50 = 1210.0 nM 5.92
CHEMBL371120 IC50 = 1770.0 nM 5.75
CHEMBL248530 IC50 = 2300.0 nM 5.64
CHEMBL245674 IC50 = 2900.0 nM 5.54
CHEMBL247720 IC50 = 3290.0 nM 5.48
CHEMBL394968 IC50 = 4560.0 nM 5.34
CHEMBL247719 Activity - -