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Assay Detail

CHEMBL4721894

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

Binding
Modulator activity at GAL4-fused human PPARdelta LBD (128 to residue at C-terminus) transfected in African green monkey CV1 cells assessed as receptor transactivation by luciferase reporter gene assay
18
Total Activities
18
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 delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective PPARδ Modulators Improve Mitochondrial Function: Potential Treatment for Duchenne Muscular Dystrophy (DMD).
Lagu B,Kluge AF,Tozzo E,Fredenburg R,Bell EL,Goddeeris MM,Dwyer P,Basinski A,Senaiar RS,Jaleel M,Tiwari NK,Panigrahi SK,Krishnamurthy NR,Takahashi T,Patane MA
ACS Med Chem Lett (2018) 9 : 935 -940
PubMed 30258544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 8.42 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755323 1 9.52
CHEMBL4649683 1 9.40
CHEMBL4640515 1 9.15
CHEMBL4739884 1 9.10
CHEMBL4743546 1 9.00
CHEMBL4740848 1 8.92
CHEMBL4741090 1 8.89
CHEMBL4744325 1 8.82
CHEMBL4757948 1 8.43
CHEMBL4764454 1 8.35
CHEMBL4784739 1 8.26
CHEMBL4740551 1 8.08
CHEMBL4757859 1 8.02
CHEMBL4755428 1 7.87
CHEMBL4739905 1 7.70
CHEMBL3958704 1 7.43
CHEMBL4748470 1 7.41
CHEMBL4753405 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755323 EC50 = 0.3 nM 9.52
CHEMBL4649683 EC50 = 0.4 nM 9.40
CHEMBL4640515 EC50 = 0.7 nM 9.15
CHEMBL4739884 EC50 = 0.8 nM 9.10
CHEMBL4743546 EC50 = 1.0 nM 9.00
CHEMBL4740848 EC50 = 1.2 nM 8.92
CHEMBL4741090 EC50 = 1.3 nM 8.89
CHEMBL4744325 EC50 = 1.5 nM 8.82
CHEMBL4757948 EC50 = 3.7 nM 8.43
CHEMBL4764454 EC50 = 4.5 nM 8.35
CHEMBL4784739 EC50 = 5.5 nM 8.26
CHEMBL4740551 EC50 = 8.4 nM 8.08
CHEMBL4757859 EC50 = 9.5 nM 8.02
CHEMBL4755428 EC50 = 13.5 nM 7.87
CHEMBL4739905 EC50 = 20.0 nM 7.70
CHEMBL3958704 EC50 = 37.0 nM 7.43
CHEMBL4748470 EC50 = 39.0 nM 7.41
CHEMBL4753405 EC50 = 59.0 nM 7.23