Tilpisertib

DB18798InvestigationalSmall molecule

Tilpisertib: Overview.

Mechanism: Pharmacologically active on Mitogen-activated protein kinase kinase kinase 8
Curator reviewed
Formula / weight: C₃₃H₃₃ClN₈O · 593.13 g/mol (avg)
Code names: GS-4875

Resolves to

Compound

Structure

InChIKeyVFGSKBLZRDRHOI-ZAGPDIDGSA-NSMILESCN1C=CC2=C(C=CC=C2C1=O)[C@H](NC1=CC2=C(NCC(C)(C)C)C(=CN=C2C(Cl)=C1)C#N)C1=CN(N=N1)C12CC(C1)C2

Targets

What you can answer from here — as of June 15, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

1Clinical trialPhase, status and sponsor resolved per trial

2+ReferencesStructured and connected to the statements they support

Which drugs share a target with Tilpisertib, and which of those have an active Phase 3 trial?

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