Delving into the Latest Updates on CFI-400936 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

TTK

Action

inhibitors

Mechanism

TTK inhibitors(Dual specificity protein kinase TTK inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

University Health Network

Active Organization-

Inactive Organization

University Health Network

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC25H27N5O3S

InChIKeyJAHXQCZCZURPTI-UHFFFAOYSA-N

CAS Registry1338793-07-9

Author: Laufer, Radoslaw ; Lin, Dan Chi-Chia ; Chirgadze, Nickolay Y ; Leung, Genie ; Lang, Yunhui ; Green, Erin ; Edwards, Louise G ; Feher, Miklos ; Beletskaya, Irina ; Wei, Xin ; Hodgson, Richard ; Luo, Xunyi ; Mak, Tak W ; Patel, Narendra Kumar B ; Li, Sze-Wan ; Harris-Brandts, Marees ; Awrey, Don E ; Plotnikova, Olga ; Ng, Grace ; Liu, Yong ; Ban, Fuqiang ; Mao, Guodong ; Qiu, Wei ; Pan, Guohua J ; Nadeem, Vincent ; Kiarash, Reza ; Huang, Ping ; Pauls, Henry W ; Mason, Jacqueline M

TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50=3.6nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.

100 Deals associated with CFI-400936

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