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Assay Detail

CHEMBL801817

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

Binding
Inhibition of [3H]ATRA binding to mouse Retinoic acid receptor RAR alpha
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Retinoic acid receptor alpha (CHEMBL2792)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure-activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity.
Muccio DD, Brouillette WJ, Alam M, Vaezi MF, Sani BP, Venepally P, Reddy L, Li E, Norris AW, Simpson-Herren L, Hill DL.
J Med Chem (1996) 39 : 3625 -3635
PubMed 8809153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.55 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38 TRETINOIN 4.0 1 8.22
CHEMBL333032 1 8.10
CHEMBL46398 1 7.96
CHEMBL705 ALITRETINOIN 4.0 1 7.51
CHEMBL122823 1 7.26
CHEMBL121659 1 6.22
CHEMBL2111792 1 -
CHEMBL2114968 1 -
CHEMBL2111790 1 -
CHEMBL2111791 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38 TRETINOIN IC50 = 6.0 nM 8.22
CHEMBL333032 IC50 = 8.0 nM 8.10
CHEMBL46398 IC50 = 11.0 nM 7.96
CHEMBL705 ALITRETINOIN IC50 = 31.0 nM 7.51
CHEMBL122823 IC50 = 55.0 nM 7.26
CHEMBL121659 IC50 = 600.0 nM 6.22
CHEMBL2111792 IC50 > 2000.0 nM -
CHEMBL2114968 IC50 > 1000.0 nM -
CHEMBL2111790 IC50 > 1000.0 nM -
CHEMBL2111791 IC50 > 2000.0 nM -