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Assay Detail

CHEMBL3227239

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

Binding
Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR alpha ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay
6
Total Activities
6
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

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

Publication

Synthetic modulators of the retinoic acid receptor-related orphan receptors
Kamenecka TM, Lyda B, Chang MR, Griffin PR
Medchemcomm (2013) 4 : 764 -776
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.34 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497207 1 7.92
CHEMBL497834 1 7.92
CHEMBL1278177 7-OXOCHOLESTEROL 1 7.92
CHEMBL62136 T091317 1 6.88
CHEMBL3094388 1 6.76
CHEMBL3218916 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497207 Ki = 12.0 nM 7.92
CHEMBL497834 Ki = 12.0 nM 7.92
CHEMBL1278177 7-OXOCHOLESTEROL Ki = 12.0 nM 7.92
CHEMBL62136 T091317 Ki = 132.0 nM 6.88
CHEMBL3094388 Ki = 172.0 nM 6.76
CHEMBL3218916 Ki = 220.0 nM 6.66