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Assay Detail

CHEMBL924747

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

Binding
Inhibition of GAL4-tagged RORalpha by luciferase assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Nuclear receptor ROR-alpha (CHEMBL5868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.
Roth J, Madoux F, Hodder P, Roush WR.
Bioorg Med Chem Lett (2008) 18 : 2628 -2632
PubMed 18374567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.88 5.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261115 1 5.78
CHEMBL261114 1 5.49
CHEMBL260419 1 4.67
CHEMBL265938 1 4.65
CHEMBL408947 1 4.60
CHEMBL411889 1 4.51
CHEMBL412079 1 4.44
CHEMBL408702 1 -
CHEMBL412080 1 -
CHEMBL261113 1 -
CHEMBL259067 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261115 IC50 = 1680.0 nM 5.78
CHEMBL261114 IC50 = 3220.0 nM 5.49
CHEMBL260419 IC50 = 21500.0 nM 4.67
CHEMBL265938 IC50 = 22600.0 nM 4.65
CHEMBL408947 IC50 = 25000.0 nM 4.60
CHEMBL411889 IC50 = 30700.0 nM 4.51
CHEMBL412079 IC50 = 36500.0 nM 4.44
CHEMBL408702 IC50 > 33000.0 nM -
CHEMBL412080 IC50 > 33000.0 nM -
CHEMBL261113 IC50 > 33000.0 nM -
CHEMBL259067 IC50 > 33000.0 nM -