Literature summary for 2.7.10.1 extracted from

Allen, J.; Bardelle, C.; Blades, K.; Buttar, D.; Chapman, L.; Colclough, N.; Dossetter, A.; Garner, A.; Girdwood, A.; Lambert, C.; Leach, A.; Law, B.; Major, J.; Plant, H.; Slater, A.
The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach (2011), Bioorg. Med. Chem. Lett., 21, 5224-5229.

Cloned(Commentary)

Cloned (Comment)	Organism
recombinant truncated enzyme	Homo sapiens

Crystallization (Commentary)

Crystallization (Comment)	Organism
molecular docking of inhibitor 2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide. The 3'-OH group acts as a hinge binder to Tyr1159 and an internal H-bond is present between the amide NH and benzyl ether oxygen. The central phenyl ring is tight against the protein surface with the basic amine side chain protruding into the solvent and near a region of acidic residues	Homo sapiens

Crystallization (Comment)

Organism

molecular docking of inhibitor 2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide. The 3'-OH group acts as a hinge binder to Tyr1159 and an internal H-bond is present between the amide NH and benzyl ether oxygen. The central phenyl ring is tight against the protein surface with the basic amine side chain protruding into the solvent and near a region of acidic residues

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
2-[(2-cyanobenzyl)oxy]-N-(3-hydroxyphenyl)-4-[3-(pyrrolidin-1-yl)propoxy]benzamide	most potent inhibitor in a series of benzanilides. Effect depends on the 3'-OH-Ph and 2''-CN-benzyl working co-operatively to deliver maximum inhibition. Modeling studies suggest a novel binding mode, incorporating a water molecule bound between these two groups and concomitant binding to the hinge	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P08581	c-Met kinase	-

Synonyms

Synonyms	Comment	Organism
c-Met receptor tyrosine kinase	-	Homo sapiens
hepatocyte growth factor receptor	-	Homo sapiens

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Release 2023.1 (January 2023)