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(4R)-4-(3-hydroxyphenyl)-N,N,7,8-tetramethyl-3,4-dihydroisoquinoline-2(1H)-carboxamide

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
01

Overview

This compound is a synthetic small molecule belonging to the class of 4-phenyltetrahydroisoquinolines. It was identified as part of a medicinal chemistry optimization effort targeting human mitotic kinesin Eg5 (also known as KIF11), an ATP-dependent motor protein essential for spindle formation during cell division. The compound acts as a potent inhibitor of Eg5 ATPase activity with an IC50 of approximately 104 nM and demonstrates anti-proliferative activity in cancer cell lines. It has been studied primarily in preclinical settings and is considered experimental; it has not advanced to clinical trials or approval for any indication[1][5][6].

Other names
(4R)-4-(3-hydroxyphenyl)-N,N,7,8-tetramethyl-1,2,3,4-tetrahydroisoquinoline-2-carboxamide(4R)-4-(3-hydroxyphényl)-N,N,7,8-tétraméthyl-3,4-dihydro-2(1H)-isoquinoléinecarboxamide(4R)-4-(3-HYDROXYPHENYL)-N,N,7,8-TETRAMETHYL-3,4-DIHYDROISOQUINOLINECARBOXAMIDE
02

Targets

KIF11 (Kinesin Spindle Protein)

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