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Assay Detail

CHEMBL4150331

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

Binding
Transactivation of human Gal4-fused RXRalpha LBD expressed in HEK293T cells after 12 to 14 hrs by dual-glo luciferase assay
10
Total Activities
10
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-alpha (CHEMBL2061)
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 10 4.92 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4171515 1 6.01
CHEMBL4167506 1 5.37
CHEMBL4163622 1 5.10
CHEMBL4173918 1 5.04
CHEMBL4174952 1 4.63
CHEMBL4163199 1 4.62
CHEMBL512164 ISOPIMARIC ACID 1 4.58
CHEMBL1545045 VALERENIC ACID 1 4.57
CHEMBL12850 DEHYDROABIETIC ACID 1 4.38
CHEMBL386313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4171515 EC50 = 970.0 nM 6.01
CHEMBL4167506 EC50 = 4300.0 nM 5.37
CHEMBL4163622 EC50 = 8000.0 nM 5.10
CHEMBL4173918 EC50 = 9100.0 nM 5.04
CHEMBL4174952 EC50 = 23600.0 nM 4.63
CHEMBL4163199 EC50 = 24000.0 nM 4.62
CHEMBL512164 ISOPIMARIC ACID EC50 = 26000.0 nM 4.58
CHEMBL1545045 VALERENIC ACID EC50 = 27000.0 nM 4.57
CHEMBL12850 DEHYDROABIETIC ACID EC50 = 42000.0 nM 4.38
CHEMBL386313 EC50 > 30000.0 nM -