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Assay Detail

CHEMBL4259388

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Binding
Agonist activity at human Gal4-fused RXRgamma expressed in HEK293T cells after 12 to 14 hrs by dual-Glo luciferase reporter gene assay
4
Total Activities
4
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

Scaffold hopping from synthetic RXR modulators by virtual screening and <i>de novo</i> design.
Merk D, Grisoni F, Friedrich L, Gelzinyte E, Schneider G.
Medchemcomm (2018) 9 : 1289 -1292
PubMed 30151082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 4.63 4.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281062 1 4.85
CHEMBL4277640 1 4.77
CHEMBL4277218 1 4.62
CHEMBL4094117 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281062 EC50 = 14100.0 nM 4.85
CHEMBL4277640 EC50 = 17000.0 nM 4.77
CHEMBL4277218 EC50 = 24000.0 nM 4.62
CHEMBL4094117 EC50 = 51000.0 nM 4.29