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Assay Detail

CHEMBL798315

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

Binding
Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]-9-cis-RA as a radioligand in baculovirus expressed receptor
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere
Vuligonda V, Lin Y, Chandraratna RA
Bioorg Med Chem Lett (1996) 6 : 213 -218
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 8.01 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69091 2 8.82
CHEMBL705 ALITRETINOIN 4.0 1 8.05
CHEMBL308883 1 7.15
CHEMBL38 TRETINOIN 4.0 1 -
CHEMBL2111535 1 -
CHEMBL2111534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69091 Kd = 1.5 nM 8.82
CHEMBL705 ALITRETINOIN Kd = 9.0 nM 8.05
CHEMBL308883 Kd = 71.0 nM 7.15
CHEMBL69091 Kd > 1000.0 nM -
CHEMBL38 TRETINOIN Kd > 1000.0 nM -
CHEMBL2111535 Kd > 1000.0 nM -
CHEMBL2111534 Kd > 1000.0 nM -