Assay Detail

CHEMBL2394936

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Binding

Binding affinity to human PPARgamma receptor by radioligand displacement assay

ChEMBL ↗

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Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235) ↗

Open DB target context

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Peroxisome proliferator-activated receptor gamma (CHEMBL235) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Peroxisome proliferator-activated receptor gamma

CHEMBL235

Anchored from Assay target.

Protein identity Peroxisome proliferator-activated receptor gamma

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.

Cappelli A, Manini M, Valenti S, Castriconi F, Giuliani G, Anzini M, Brogi S, Butini S, Gemma S, Campiani G, Giorgi G, Mennuni L, Lanza M, Giordani A, Caselli G, Letari O, Makovec F.
Eur J Med Chem (2013) 63 : 85 -94
PubMed 23466604 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	8.24	8.24
IC50	1	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL121	ROSIGLITAZONE	4.0	2	8.24

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL121	ROSIGLITAZONE	Ki	=	5.8	nM	8.24
CHEMBL121	ROSIGLITAZONE	IC50	=	11.0	nM	7.96