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Assay Detail

CHEMBL799703

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

Binding
Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR alpha
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Retinoic acid receptor ligands based on the 6-cyclopropyl-2,4-hexadienoic acid.
Farmer LJ, Zhi L, Jeong S, Lamph WW, Osburn DL, Croston G, Flatten KS, Heyman RA, Nadzan AM.
Bioorg Med Chem Lett (2003) 13 : 261 -264
PubMed 12482435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.60 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89331 1 7.23
CHEMBL705 ALITRETINOIN 4.0 1 6.66
CHEMBL38 TRETINOIN 4.0 1 6.36
CHEMBL89581 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89331 EC50 = 59.0 nM 7.23
CHEMBL705 ALITRETINOIN EC50 = 220.0 nM 6.66
CHEMBL38 TRETINOIN EC50 = 436.0 nM 6.36
CHEMBL89581 EC50 = 733.0 nM 6.13