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Assay Detail

CHEMBL4222297

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

Binding
Displacement of [3H]-T0901317 from recombinant human His-SUMO-tagged RORgamma LBD (265 to 518 residues) expressed in Escherichia coli BL21(DE3) at after 1 hr by scintillation proximity assay
33
Total Activities
33
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-gamma (CHEMBL1741186)
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
IC50 33 5.85 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4225808 1 7.89
CHEMBL4227134 1 4.87
CHEMBL4227867 1 4.79
CHEMBL4229015 1 -
CHEMBL4228180 1 -
CHEMBL4229273 1 -
CHEMBL4227984 1 -
CHEMBL4228496 1 -
CHEMBL4227659 1 -
CHEMBL4228755 1 -
CHEMBL4226645 1 -
CHEMBL4226607 1 -
CHEMBL4227452 1 -
CHEMBL4227190 1 -
CHEMBL4226929 1 -
CHEMBL4226875 1 -
CHEMBL4226846 1 -
CHEMBL4225264 1 -
CHEMBL4228315 1 -
CHEMBL4225424 1 -
CHEMBL4228577 1 -
CHEMBL4228640 1 -
CHEMBL4226086 1 -
CHEMBL4227974 1 -
CHEMBL4228057 1 -
CHEMBL4226392 1 -
CHEMBL4225557 1 -
CHEMBL4226667 1 -
CHEMBL4225823 1 -
CHEMBL4227792 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4225808 IC50 = 13.0 nM 7.89
CHEMBL4227134 IC50 = 13400.0 nM 4.87
CHEMBL4227867 IC50 = 16100.0 nM 4.79
CHEMBL4226929 IC50 - -
CHEMBL4226071 IC50 > 40000.0 nM -
CHEMBL4227190 IC50 > 40000.0 nM -
CHEMBL4227452 IC50 - -
CHEMBL4226607 IC50 - -
CHEMBL4226645 IC50 > 40000.0 nM -
CHEMBL4228755 IC50 - -
CHEMBL4227659 IC50 - -
CHEMBL4228496 IC50 - -
CHEMBL4227984 IC50 - -
CHEMBL4229273 IC50 > 40000.0 nM -
CHEMBL4228180 IC50 - -
CHEMBL4229015 IC50 - -
CHEMBL4227179 IC50 - -
CHEMBL4225309 IC50 - -
CHEMBL4226875 IC50 - -
CHEMBL4226846 IC50 - -
CHEMBL4225264 IC50 > 40000.0 nM -
CHEMBL4228315 IC50 - -
CHEMBL4225424 IC50 - -
CHEMBL4228577 IC50 > 40000.0 nM -
CHEMBL4228640 IC50 > 40000.0 nM -
CHEMBL4226086 IC50 - -
CHEMBL4227974 IC50 - -
CHEMBL4228057 IC50 > 40000.0 nM -
CHEMBL4226392 IC50 > 40000.0 nM -
CHEMBL4225557 IC50 - -
CHEMBL4226667 IC50 - -
CHEMBL4225823 IC50 > 40000.0 nM -
CHEMBL4227792 IC50 - -