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Assay Detail

CHEMBL4018944

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

Binding
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD by TR-FRET assay
8
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.
Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M.
J Med Chem (2017) 60 : 7459 -7475
PubMed 28799755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.05 10.30
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434063 1 10.30
CHEMBL594625 1 9.77
CHEMBL603424 1 8.74
CHEMBL431733 NAMODENOSON 3.0 2 8.66
CHEMBL413686 2 8.47
CHEMBL200732 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434063 Ki = 0.0497 nM 10.30
CHEMBL594625 Ki = 0.17 nM 9.77
CHEMBL603424 Ki = 1.83 nM 8.74
CHEMBL431733 NAMODENOSON Ki = 2.18 nM 8.66
CHEMBL413686 Ki = 3.42 nM 8.47
CHEMBL200732 Ki = 4.6 nM 8.34
CHEMBL413686 Inhibition - % -
CHEMBL431733 NAMODENOSON Inhibition - % -