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CRA_1144

Development stage: Preclinical
Lead developer: Pfizer
Modality: Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules

Overview

CRA_1144 is a small molecule inhibitor belonging to the phenylbenzimidazole class of organic compounds. It is characterized chemically as 2-{5-[amino(imino)methyl]-1H-benzimidazol-2-yl}benzenolate with the formula C14H12N4O. The compound acts as an inhibitor of serine protease hepsin (HPN), a target implicated in cancer progression and metastasis. Its mechanism involves binding to the active site of hepsin via a multi-centered short hydrogen bonding network. CRA_1144 has been primarily used as a discovery agent and investigative tool in research settings rather than for clinical therapy[1][3][7].

Other names: CRA_1144AC1O4QI2AC-1O4QI2AC 1O4QI2PD006741PD-006741PD 006741

Targets

HPN (Hepsin)

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