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Assay Detail

CHEMBL772308

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

Binding
Transcriptional activation for RAR alpha receptor
9
Total Activities
9
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 alpha (CHEMBL2055)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural basis for the differential RXR & RAR activity of stilbene retinoid analogs
Beard RL, Gil DW, Marler DK, Henry E, Colon DF, Gillett SJ, Arefieg T, Breen TS, Krauss H, Davies PJ, Chandraratna RA
Bioorg Med Chem Lett (1994) 4 : 1447 -1452
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.21 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38 TRETINOIN 4.0 1 8.30
CHEMBL12585 1 7.96
CHEMBL441231 1 7.82
CHEMBL275311 1 7.68
CHEMBL285179 1 7.62
CHEMBL705 ALITRETINOIN 4.0 1 6.99
CHEMBL284167 1 6.00
CHEMBL32505 1 5.34
CHEMBL36464 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38 TRETINOIN EC50 = 5.0 nM 8.30
CHEMBL12585 EC50 = 11.0 nM 7.96
CHEMBL441231 EC50 = 15.0 nM 7.82
CHEMBL275311 EC50 = 21.0 nM 7.68
CHEMBL285179 EC50 = 24.0 nM 7.62
CHEMBL705 ALITRETINOIN EC50 = 102.0 nM 6.99
CHEMBL284167 EC50 = 989.0 nM 6.00
CHEMBL32505 EC50 = 4580.0 nM 5.34
CHEMBL36464 EC50 > 1000.0 nM -