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Assay Detail

CHEMBL4150337

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

Binding
Transactivation of human Gal4-fused RXRgamma LBD expressed in HEK293T cells after 12 to 14 hrs by dual-glo luciferase assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Retinoic acid receptor RXR-gamma (CHEMBL2004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Computer-Assisted Discovery of Retinoid X Receptor Modulating Natural Products and Isofunctional Mimetics.
Merk D, Grisoni F, Friedrich L, Gelzinyte E, Schneider G.
J Med Chem (2018) 61 : 5442 -5447
PubMed 29901398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 4.74 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173918 1 5.60
CHEMBL4171515 1 5.47
CHEMBL4163622 1 4.85
CHEMBL4167506 1 4.61
CHEMBL4174952 1 4.57
CHEMBL512164 ISOPIMARIC ACID 1 4.48
CHEMBL12850 DEHYDROABIETIC ACID 1 4.38
CHEMBL1545045 VALERENIC ACID 1 4.37
CHEMBL4163199 1 4.30
CHEMBL4162951 1 -
CHEMBL294740 SCLAREOL 1 -
CHEMBL2147421 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173918 EC50 = 2500.0 nM 5.60
CHEMBL4171515 EC50 = 3400.0 nM 5.47
CHEMBL4163622 EC50 = 14000.0 nM 4.85
CHEMBL4167506 EC50 = 24800.0 nM 4.61
CHEMBL4174952 EC50 = 27200.0 nM 4.57
CHEMBL512164 ISOPIMARIC ACID EC50 = 33000.0 nM 4.48
CHEMBL12850 DEHYDROABIETIC ACID EC50 = 42000.0 nM 4.38
CHEMBL1545045 VALERENIC ACID EC50 = 43000.0 nM 4.37
CHEMBL4163199 EC50 = 50000.0 nM 4.30
CHEMBL4162951 EC50 - -
CHEMBL294740 SCLAREOL EC50 - -
CHEMBL2147421 EC50 - -