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Assay Detail

CHEMBL756485

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

Functional
In vitro transactivation of Peroxisome proliferator activated receptor alpha.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.
Collins JL, Blanchard SG, Boswell GE, Charifson PS, Cobb JE, Henke BR, Hull-Ryde EA, Kazmierski WM, Lake DH, Leesnitzer LM, Lehmann J, Lenhard JM, Orband-Miller LA, Gray-Nunez Y, Parks DJ, Plunkett KD, Tong WQ.
J Med Chem (1998) 41 : 5037 -5054
PubMed 9836621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.03 6.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147384 1 6.59
CHEMBL356382 1 6.41
CHEMBL107367 FARGLITAZAR 2.0 1 6.34
CHEMBL147095 1 6.24
CHEMBL148797 1 6.18
CHEMBL358379 1 5.98
CHEMBL343210 1 5.74
CHEMBL148459 1 5.56
CHEMBL358325 1 5.19
CHEMBL149715 1 -
CHEMBL147935 1 -
CHEMBL146806 1 -
CHEMBL146301 1 -
CHEMBL148950 1 -
CHEMBL146650 1 -
CHEMBL146231 1 -
CHEMBL446629 1 -
CHEMBL149876 1 -
CHEMBL359285 1 -
CHEMBL356707 1 -
CHEMBL342292 1 -
CHEMBL149835 1 -
CHEMBL147090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147384 EC50 = 257.04 nM 6.59
CHEMBL356382 EC50 = 389.05 nM 6.41
CHEMBL107367 FARGLITAZAR EC50 = 457.09 nM 6.34
CHEMBL147095 EC50 = 575.44 nM 6.24
CHEMBL148797 EC50 = 660.69 nM 6.18
CHEMBL358379 EC50 = 1047.13 nM 5.98
CHEMBL343210 EC50 = 1819.7 nM 5.74
CHEMBL148459 EC50 = 2754.23 nM 5.56
CHEMBL358325 EC50 = 6456.54 nM 5.19
CHEMBL149715 EC50 < 10000.0 nM -
CHEMBL147935 EC50 < 10000.0 nM -
CHEMBL146806 EC50 < 10000.0 nM -
CHEMBL146301 EC50 < 10000.0 nM -
CHEMBL148950 EC50 < 10000.0 nM -
CHEMBL146650 EC50 < 10000.0 nM -
CHEMBL146231 EC50 < 10000.0 nM -
CHEMBL446629 EC50 < 10000.0 nM -
CHEMBL149876 EC50 < 10000.0 nM -
CHEMBL359285 EC50 < 10000.0 nM -
CHEMBL356707 EC50 < 10000.0 nM -
CHEMBL342292 EC50 < 10000.0 nM -
CHEMBL149835 EC50 < 10000.0 nM -
CHEMBL147090 EC50 < 10000.0 nM -