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Assay Detail

CHEMBL5732271

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

Binding
Retinoid Nuclear Receptor Activity: Retinoid nuclear receptor activity is associated with transduction of the non-visual physiologic, pharmacologic, and toxicologic retinoid signals that affect tissue and organ growth, development, differentiation, and homeostasis.The effect of the Compounds of Examples 4, 28, and 29 (Compound 4, Compound 28, and Compound 29) and the effect of a retinoic acid receptor (RAR) agonist (E-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl]benzoic acid) (TTNPB), and of all-trans-retinoic acid (at-RA), which is an RAR and retinoid X receptor (RXR) agonist, were studied on RAR and RXR receptors essentially as described by Achkar et al. (Proc. Natl. Acad. Sci. USA 93:4879-84 (1996)). Results of these assays are presented in Table 11. Amounts as great as 10 μM of each of Compound 4-HCl, Compound 28-HCl, and Compound 29-HCl did not show any significant effects on retinoid nuclear receptors (RAR and RXR)
3
Total Activities
1
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor gamma (CHEMBL2003)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alkoxy compounds for disease treatment
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 10.19 10.19
kon 1 - -
k_off 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5997757 3 10.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5997757 EC50 = 0.065 nM 10.19
CHEMBL5997757 kon = - -
CHEMBL5997757 k_off = - s-1 -