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Assay Detail

CHEMBL759401

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

Binding
Binding affinity for human PPAR delta receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.
Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR, Sternbach DD.
Bioorg Med Chem Lett (2003) 13 : 1517 -1521
PubMed 12699745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38508 1 9.00
CHEMBL38943 GW501516 2.0 1 9.00
CHEMBL289887 1 8.52
CHEMBL288341 1 7.52
CHEMBL37013 1 7.52
CHEMBL39894 1 7.22
CHEMBL37495 1 7.05
CHEMBL39687 1 7.05
CHEMBL416794 1 6.47
CHEMBL40614 1 6.00
CHEMBL39129 1 6.00
CHEMBL36268 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38508 IC50 = 1.0 nM 9.00
CHEMBL38943 GW501516 IC50 = 1.0 nM 9.00
CHEMBL289887 IC50 = 3.0 nM 8.52
CHEMBL288341 IC50 = 30.0 nM 7.52
CHEMBL37013 IC50 = 30.0 nM 7.52
CHEMBL39894 IC50 = 60.0 nM 7.22
CHEMBL37495 IC50 = 90.0 nM 7.05
CHEMBL39687 IC50 = 90.0 nM 7.05
CHEMBL416794 IC50 = 340.0 nM 6.47
CHEMBL40614 IC50 = 1000.0 nM 6.00
CHEMBL39129 IC50 = 1000.0 nM 6.00
CHEMBL36268 IC50 = 5500.0 nM 5.26