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Assay Detail

CHEMBL3077607

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

Binding
Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay
ChEMBL ↗
50
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

3D-QSAR study of tyrosine and propanoic acid derivatives as PPAR/ dual agonists using CoMSIA
Verma RK, Kumar V, Ghosh P, Wadhwa LK
Med Chem Res (2013) 22 : 287 -302
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 50 6.10 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2237300 — — 2 9.00
CHEMBL81248 — — 2 8.30
CHEMBL77502 LY-510929 — 2 8.05
CHEMBL355695 — — 2 6.66
CHEMBL87307 — — 2 6.52
CHEMBL86658 — — 2 6.44
CHEMBL2282523 — — 2 6.34
CHEMBL421729 — — 2 6.16
CHEMBL87380 — — 2 6.16
CHEMBL420973 — — 2 6.05
CHEMBL2282517 — — 2 5.98
CHEMBL89152 — — 2 5.96
CHEMBL2282519 — — 2 5.89
CHEMBL86688 — — 2 5.66
CHEMBL328099 — — 2 5.66
CHEMBL167430 — — 2 5.62
CHEMBL315048 — — 2 5.50
CHEMBL24038 RAGAGLITAZAR 2.0 2 5.49
CHEMBL2282520 — — 2 5.46
CHEMBL2282522 — — 2 5.44
CHEMBL86657 — — 2 5.35
CHEMBL327481 — — 2 5.28
CHEMBL314483 — — 2 5.19
CHEMBL2282518 — — 2 5.19
CHEMBL2282521 — — 2 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2237300 — EC50 = 1.0 nM 9.00
CHEMBL2237300 — EC50 = 1.0 nM 9.00
CHEMBL81248 — EC50 = 5.012 nM 8.30
CHEMBL81248 — EC50 = 5.0 nM 8.30
CHEMBL77502 LY-510929 EC50 = 9.0 nM 8.05
CHEMBL77502 LY-510929 EC50 = 8.913 nM 8.05
CHEMBL355695 — EC50 = 218.78 nM 6.66
CHEMBL355695 — EC50 = 220.0 nM 6.66
CHEMBL87307 — EC50 = 300.0 nM 6.52
CHEMBL87307 — EC50 = 302.0 nM 6.52
CHEMBL86658 — EC50 = 360.0 nM 6.44
CHEMBL86658 — EC50 = 363.08 nM 6.44
CHEMBL2282523 — EC50 = 457.0 nM 6.34
CHEMBL2282523 — EC50 = 457.09 nM 6.34
CHEMBL421729 — EC50 = 700.0 nM 6.16
CHEMBL87380 — EC50 = 691.83 nM 6.16
CHEMBL421729 — EC50 = 691.83 nM 6.16
CHEMBL87380 — EC50 = 700.0 nM 6.16
CHEMBL420973 — EC50 = 891.25 nM 6.05
CHEMBL420973 — EC50 = 900.0 nM 6.05
CHEMBL2282517 — EC50 = 1047.0 nM 5.98
CHEMBL2282517 — EC50 = 1047.13 nM 5.98
CHEMBL89152 — EC50 = 1096.48 nM 5.96
CHEMBL89152 — EC50 = 1100.0 nM 5.96
CHEMBL2282519 — EC50 = 1288.25 nM 5.89
CHEMBL2282519 — EC50 = 1300.0 nM 5.89
CHEMBL86688 — EC50 = 2200.0 nM 5.66
CHEMBL86688 — EC50 = 2187.76 nM 5.66
CHEMBL328099 — EC50 = 2200.0 nM 5.66
CHEMBL328099 — EC50 = 2187.76 nM 5.66
CHEMBL167430 — EC50 = 2400.0 nM 5.62
CHEMBL167430 — EC50 = 2398.83 nM 5.62
CHEMBL315048 — EC50 = 3200.0 nM 5.50
CHEMBL315048 — EC50 = 3162.28 nM 5.50
CHEMBL24038 RAGAGLITAZAR EC50 = 3235.94 nM 5.49
CHEMBL24038 RAGAGLITAZAR EC50 = 3210.0 nM 5.49
CHEMBL2282520 — EC50 = 3467.37 nM 5.46
CHEMBL2282520 — EC50 = 3500.0 nM 5.46
CHEMBL2282522 — EC50 = 3600.0 nM 5.44
CHEMBL2282522 — EC50 = 3630.78 nM 5.44
CHEMBL86657 — EC50 = 4500.0 nM 5.35
CHEMBL86657 — EC50 = 4466.84 nM 5.35
CHEMBL327481 — EC50 = 5300.0 nM 5.28
CHEMBL327481 — EC50 = 5248.07 nM 5.28
CHEMBL314483 — EC50 = 6400.0 nM 5.19
CHEMBL2282518 — EC50 = 6456.0 nM 5.19
CHEMBL314483 — EC50 = 6456.54 nM 5.19
CHEMBL2282518 — EC50 = 6456.54 nM 5.19
CHEMBL2282521 — EC50 = 6900.0 nM 5.16
CHEMBL2282521 — EC50 = 6918.31 nM 5.16