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Assay Detail

CHEMBL1780401

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Functional
Agonist activity at Gal4-fussed PPARdelta expressed in human HEK293 cells by reporter gene assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design, synthesis, and nonalcoholic steatohepatitis (NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator-activated receptor (PPAR) α-selective agonists.
Ban S, Kasuga J, Nakagome I, Nobusada H, Takayama F, Hirono S, Kawasaki H, Hashimoto Y, Miyachi H.
Bioorg Med Chem (2011) 19 : 3183 -3191
PubMed 21530275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.11 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1779473 1 6.96
CHEMBL1222408 1 6.92
CHEMBL270587 1 6.68
CHEMBL1779480 1 6.52
CHEMBL255392 1 6.44
CHEMBL1779481 1 6.24
CHEMBL1779482 1 6.10
CHEMBL1779478 1 5.85
CHEMBL1779479 1 5.85
CHEMBL1779476 1 5.39
CHEMBL1779474 1 5.32
CHEMBL255593 1 5.09
CHEMBL1779475 1 -
CHEMBL1779477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1779473 EC50 = 110.0 nM 6.96
CHEMBL1222408 EC50 = 120.0 nM 6.92
CHEMBL270587 EC50 = 210.0 nM 6.68
CHEMBL1779480 EC50 = 300.0 nM 6.52
CHEMBL255392 EC50 = 360.0 nM 6.44
CHEMBL1779481 EC50 = 580.0 nM 6.24
CHEMBL1779482 EC50 = 800.0 nM 6.10
CHEMBL1779478 EC50 = 1400.0 nM 5.85
CHEMBL1779479 EC50 = 1400.0 nM 5.85
CHEMBL1779476 EC50 = 4100.0 nM 5.39
CHEMBL1779474 EC50 = 4800.0 nM 5.32
CHEMBL255593 EC50 = 8100.0 nM 5.09
CHEMBL1779475 EC50 > 10000.0 nM -
CHEMBL1779477 EC50 > 10000.0 nM -