Assay Detail

CHEMBL797870

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Functional

Agonistic activity towards retinoic acid receptor-gamma

ChEMBL ↗

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Target

Retinoic acid receptor gamma (CHEMBL2003) ↗

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Primary target Retinoic acid receptor gamma

CHEMBL2003

Anchored from Assay target.

Protein identity Retinoic acid 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	Functional
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Expert

Target

Retinoic acid receptor gamma (CHEMBL2003) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Regulation of retinoidal actions by diazepinylbenzoic acids. Retinoid synergists which activate the RXR-RAR heterodimers.

Umemiya H, Fukasawa H, Ebisawa M, Eyrolles L, Kawachi E, Eisenmann G, Gronemeyer H, Hashimoto Y, Shudo K, Kagechika H.
J Med Chem (1997) 40 : 4222 -4234
PubMed 9435893 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	9.70	10.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL38	TRETINOIN	4.0	1	10.40
CHEMBL705	ALITRETINOIN	4.0	1	9.00

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL38	TRETINOIN	Ki	=	0.04	nM	10.40
CHEMBL705	ALITRETINOIN	Ki	=	1.0	nM	9.00