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Assay Detail

CHEMBL799719

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

Binding
Binding affinity towards retinoic acid receptor alpha was determined using [3H]ATRA (5 nM) as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor alpha (CHEMBL2055)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Beard RL, Klein ES, Standeven AM, Escobar M, Chandraratna RA.
Bioorg Med Chem Lett (2001) 11 : 765 -768
PubMed 11277515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.12 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38 TRETINOIN 4.0 1 7.85
CHEMBL358145 1 7.77
CHEMBL165843 1 7.44
CHEMBL350485 1 6.89
CHEMBL349935 1 6.87
CHEMBL151870 1 6.87
CHEMBL349018 1 6.83
CHEMBL424190 1 6.46
CHEMBL164176 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38 TRETINOIN Kd = 14.0 nM 7.85
CHEMBL358145 Kd = 17.0 nM 7.77
CHEMBL165843 Kd = 36.0 nM 7.44
CHEMBL350485 Kd = 129.0 nM 6.89
CHEMBL349935 Kd = 136.0 nM 6.87
CHEMBL151870 Kd = 135.0 nM 6.87
CHEMBL349018 Kd = 148.0 nM 6.83
CHEMBL424190 Kd = 350.0 nM 6.46
CHEMBL164176 Kd > 1000.0 nM -