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Assay Detail

CHEMBL896364

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Functional
Agonist activity at human PPARdelta expressed in HepG2 cells after 16 hrs by luciferase reporter gene assay
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery of highly potent and selective benzyloxybenzyl-based peroxisome proliferator-activator receptor (PPAR) delta agonists.
Bratton LD, Filzen GF, Geyer A, Hoffman JK, Lu G, Pulaski J, Trivedi BK, Unangst PC, Xu X.
Bioorg Med Chem Lett (2007) 17 : 3624 -3629
PubMed 17498950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.28 7.89
IC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234659 1 7.89
CHEMBL232400 1 7.16
CHEMBL234665 1 6.64
CHEMBL234660 1 6.60
CHEMBL232397 1 6.60
CHEMBL392949 1 6.57
CHEMBL232395 1 6.53
CHEMBL391478 1 6.43
CHEMBL233177 1 6.28
CHEMBL232398 1 6.23
CHEMBL234661 1 6.03
CHEMBL392950 1 5.76
CHEMBL234662 1 5.71
CHEMBL234663 1 5.66
CHEMBL267147 1 5.58
CHEMBL232399 1 4.87
CHEMBL232396 1 -
CHEMBL391479 1 -
CHEMBL234666 1 -
CHEMBL392951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234659 EC50 = 13.0 nM 7.89
CHEMBL232400 EC50 = 70.0 nM 7.16
CHEMBL234665 EC50 = 230.0 nM 6.64
CHEMBL234660 EC50 = 252.0 nM 6.60
CHEMBL232397 EC50 = 251.0 nM 6.60
CHEMBL392949 EC50 = 267.0 nM 6.57
CHEMBL232395 EC50 = 295.0 nM 6.53
CHEMBL391478 EC50 = 374.0 nM 6.43
CHEMBL233177 EC50 = 530.0 nM 6.28
CHEMBL232398 EC50 = 585.0 nM 6.23
CHEMBL234661 EC50 = 933.0 nM 6.03
CHEMBL392950 EC50 = 1720.0 nM 5.76
CHEMBL234662 EC50 = 1970.0 nM 5.71
CHEMBL234663 EC50 = 2210.0 nM 5.66
CHEMBL267147 EC50 = 2610.0 nM 5.58
CHEMBL232399 EC50 = 13600.0 nM 4.87
CHEMBL232396 IC50 > 10000.0 nM -
CHEMBL391479 IC50 > 10000.0 nM -
CHEMBL234666 EC50 - -
CHEMBL392951 EC50 - -