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Assay Detail

CHEMBL798316

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

Binding
Inhibition of [3H]9-cis-RA binding to RXR alpha receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of potent conformationally restricted retinoid X receptor ligands
Farmer LJ, Lin Zhi, Susan Jeong, Adam Kallel E, Croston G, Flatten KS, Heyman RA, Nadzan AM
Bioorg Med Chem Lett (1997) 7 : 2747 -2752
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.73 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93518 1 8.52
CHEMBL92284 1 8.40
CHEMBL1023 BEXAROTENE 4.0 1 7.85
CHEMBL93848 1 7.04
CHEMBL96184 1 6.82
CHEMBL92394 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93518 Ki = 3.0 nM 8.52
CHEMBL92284 Ki = 4.0 nM 8.40
CHEMBL1023 BEXAROTENE Ki = 14.0 nM 7.85
CHEMBL93848 Ki = 92.0 nM 7.04
CHEMBL96184 Ki = 150.0 nM 6.82
CHEMBL92394 Ki > 1000.0 nM -