RORα and RORα/γ Inverse Agonist Probes

CID/MLTarget NameIC50 (nM) [SID, AID]Anti-targetIC50 (μM) [SID, AID]Fold SelectiveSecondary Assays: IC50 (nM) [SID, AID]
PROBE 1 CID-447912/ML125:RORαIC50: 2000 nM [SID-85257301, AID-2117]VP16Inactive at 10 μM [SID-85257301, AID-2117]Dual RORα RORγ Inverse Agonist
RORγIC50: 1730 nM [SID-85257301, AID-2117]
PROBE 2: CID-44237404/ML124RORαIC50: 2470 nM [SID-85257298, AID-2117]VP16Inactive at 10 μM [SID-85257298, AID-2117]Selective RORα Inverse Agonist
RORγRORγ IC50: > 20 μM (Inactive)

From: Campaign to identify novel modulators of the Retinoic acid receptor-related Orphan Receptors (ROR)

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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