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Assay Detail

CHEMBL4222299

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

Binding
Inverse agonist activity at GAL4-DNA binding domain-fused human RORbeta ligand binding domain expressed in HEK293T cells incubated for 20 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
2
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-beta (CHEMBL3091268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of an aminothiazole series of RORβ modulators.
Patouret R, Doebelin C, Garcia-Ordonez RD, Chang MR, Ruiz C, Cameron MD, Griffin PR, Kamenecka TM.
Bioorg Med Chem Lett (2018) 28 : 1178 -1181
PubMed 29534930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 4 - -
IC50 1 6.07 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4225808 1 6.07
CHEMBL4226071 1 -
CHEMBL4226645 1 -
CHEMBL4225264 1 -
CHEMBL4227867 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4225808 IC50 = 860.0 nM 6.07
CHEMBL4226071 Activity - -
CHEMBL4226645 Activity - -
CHEMBL4225264 Activity - -
CHEMBL4227867 Activity - -