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Assay Detail

CHEMBL804950

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

Binding
Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor gamma using transactivation assay
7
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Retinoic acid receptor gamma (CHEMBL2003)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere
Vuligonda V, Lin Y, Chandraratna RA
Bioorg Med Chem Lett (1996) 6 : 213 -218
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.73 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38 TRETINOIN 4.0 1 9.15
CHEMBL705 ALITRETINOIN 4.0 1 7.35
CHEMBL69091 2 6.70
CHEMBL308883 1 -
CHEMBL2111535 1 -
CHEMBL2111534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38 TRETINOIN EC50 = 0.7 nM 9.15
CHEMBL705 ALITRETINOIN EC50 = 45.0 nM 7.35
CHEMBL69091 EC50 = 200.0 nM 6.70
CHEMBL308883 EC50 > 1000.0 nM -
CHEMBL69091 EC50 > 1000.0 nM -
CHEMBL2111535 EC50 > 1000.0 nM -
CHEMBL2111534 EC50 > 1000.0 nM -