Literature summary for 2.7.10.1 extracted from

Weiss, M.M.; Harmange, J.C.; Polverino, A.J.; Bauer, D.; Berry, L.; Berry, V.; Borg, G.; Bready, J.; Chen, D.; Choquette, D.; Coxon, A.; DeMelfi, T.; Doerr, N.; Estrada, J.; Flynn, J.; Graceffa, R.F.; Harriman, S.P.; Kaufman, S.; La, D.S.; Long, A.; Neervannan, S.; Patel, V.F.; Potashman, M.; Regal, K.; Rove, R.o.v.e.t.
Evaluation of a series of naphthamides as potent, orally active vascular endothelial growth factor receptor-2 tyrosine kinase inhibitors (2008), J. Med. Chem., 51, 1668-1680.

Application

Application	Comment	Organism
drug development	N-alkyl and N-unsubstituted naphthamides are potent and selective inhibitors of KDR	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide	-	Homo sapiens
4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide	-	Homo sapiens
4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide	-	Homo sapiens
6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide	-	Homo sapiens
6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide	-	Homo sapiens
6-(7-methoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens
N-tert-butyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P35968	-	-

Synonyms

Synonyms	Comment	Organism
KDR	-	Homo sapiens
vascular endothelial growth factor receptor	-	Homo sapiens
VEGFR-2	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.00000037	-	-	Homo sapiens	4-(5-(cyclopropylcarbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
0.00000045	-	-	Homo sapiens	N-cyclopropyl-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
0.0000006	-	-	Homo sapiens	N-cyclopropyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000009	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide methanesulfonate
0.0000012	-	-	Homo sapiens	6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
0.0000013	-	-	Homo sapiens	N-cyclobutyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.0000013	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-propyl-1-naphthamide
0.0000013	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-ethyl-1-naphthamide
0.0000013	-	-	Homo sapiens	6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
0.0000013	-	-	Homo sapiens	4-(5-carbamoylnaphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
0.0000029	-	-	Homo sapiens	N-cyclopropyl-6-(6,7-dimethoxyquinazolin-4-yloxy)-1-naphthamide
0.0000038	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-methyl-1-naphthamide
0.0000038	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2,2,2-trifluoroethyl)-1-naphthamide
0.0000042	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-(3-methoxypropyl)-1-naphthamide
0.0000059	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-isopropyl-1-naphthamide
0.000011	-	-	Homo sapiens	N-(cyclopropylmethyl)-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000012	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
0.000015	-	-	Homo sapiens	N-cyclopentyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide
0.000015	-	-	Homo sapiens	6-(6,7-dimethoxyquinolin-4-yloxy)-N-(1-methylcyclopropyl)-1-naphthamide
0.000022	-	-	Homo sapiens	4-(5-((2-methoxyethyl)carbamoyl)naphthalen-2-yloxy)-7-methoxyquinoline-6-carboxamide
0.000028	-	-	Homo sapiens	N-(2-methoxyethyl)-6-(7-methoxyquinolin-4-yloxy)-1-naphthamide
0.000314	-	-	Homo sapiens	6-(6,7-dimethoxyquinazolin-4-yloxy)-N-(2-methoxyethyl)-1-naphthamide
0.0015	-	-	Homo sapiens	N-tert-butyl-6-(6,7-dimethoxyquinolin-4-yloxy)-1-naphthamide