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Assay Detail

CHEMBL799869

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Functional
Antagonist activity of TTNPB (10 nM) function at retinoic acid receptor alpha
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
IC50 5 6.71 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358145 1 7.51
CHEMBL349018 1 6.68
CHEMBL349935 1 6.66
CHEMBL350485 1 6.65
CHEMBL424190 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358145 IC50 = 31.0 nM 7.51
CHEMBL349018 IC50 = 210.0 nM 6.68
CHEMBL349935 IC50 = 220.0 nM 6.66
CHEMBL350485 IC50 = 225.0 nM 6.65
CHEMBL424190 IC50 = 875.0 nM 6.06