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Assay Detail

CHEMBL800761

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

Binding
Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR gamma
20
Total Activities
20
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-gamma (CHEMBL4402)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids.
Boehm MF, Zhang L, Badea BA, White SK, Mais DE, Berger E, Suto CM, Goldman ME, Heyman RA.
J Med Chem (1994) 37 : 2930 -2941
PubMed 8071941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 20 6.74 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1023 BEXAROTENE 4.0 1 7.54
CHEMBL101661 1 7.46
CHEMBL101609 1 7.36
CHEMBL100623 1 7.23
CHEMBL330593 1 7.03
CHEMBL101212 1 6.95
CHEMBL102039 1 6.87
CHEMBL99325 1 6.85
CHEMBL101712 1 6.82
CHEMBL96184 1 6.54
CHEMBL101666 1 6.51
CHEMBL101302 1 6.48
CHEMBL97910 1 6.37
CHEMBL98172 1 6.37
CHEMBL98142 1 6.15
CHEMBL328419 1 6.09
CHEMBL419166 1 6.04
CHEMBL318916 1 -
CHEMBL100986 1 -
CHEMBL101308 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1023 BEXAROTENE Kd = 29.0 nM 7.54
CHEMBL101661 Kd = 35.0 nM 7.46
CHEMBL101609 Kd = 44.0 nM 7.36
CHEMBL100623 Kd = 59.0 nM 7.23
CHEMBL330593 Kd = 94.0 nM 7.03
CHEMBL101212 Kd = 113.0 nM 6.95
CHEMBL102039 Kd = 135.0 nM 6.87
CHEMBL99325 Kd = 142.0 nM 6.85
CHEMBL101712 Kd = 150.0 nM 6.82
CHEMBL96184 Kd = 290.0 nM 6.54
CHEMBL101666 Kd = 309.0 nM 6.51
CHEMBL101302 Kd = 332.0 nM 6.48
CHEMBL97910 Kd = 424.0 nM 6.37
CHEMBL98172 Kd = 424.0 nM 6.37
CHEMBL98142 Kd = 704.0 nM 6.15
CHEMBL328419 Kd = 812.0 nM 6.09
CHEMBL419166 Kd = 911.0 nM 6.04
CHEMBL318916 Kd > 1000.0 nM -
CHEMBL100986 Kd > 1000.0 nM -
CHEMBL101308 Kd > 1000.0 nM -