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Literature summary for 2.7.10.1 extracted from

  • Barlaam, B.; Ballard, P.; Bradbury, R.H.; Ducray, R.; Germain, H.; Hickinson, D.M.; Hudson, K.; Kettle, J.G.; Klinowska, T.; Magnien, F.; Ogilvie, D.J.; Olivier, A.; Pearson, S.E.; Scott, J.S.; Suleman, A.; Trigwell, C.B.; Vautier, M.; Whittaker, R.D.; Wood, R.
    A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase (2008), Bioorg. Med. Chem. Lett., 18, 674-678.
    View publication on PubMed
Search for more literature for 2.7.10.1

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
 Homo sapiens
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
 Homo sapiens
(2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
 Homo sapiens
(2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
(2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
(2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
(2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
 Homo sapiens
(2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
-
 Homo sapiens
(2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
(2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
-
 Homo sapiens
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
-
 Homo sapiens
2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]acetamide
-
 Homo sapiens
N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
-
 Homo sapiens
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine
-
 Homo sapiens
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens
N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens
N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens
N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens
N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
KB cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
erbB2 receptor tyrosine kinase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
0.000022
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
0.000023
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.000023
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-methoxy-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
0.000027
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-chloro-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
0.00003
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.000031
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
0.000034
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.000035
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]-5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
0.000043
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.000066
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
0.000069
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.000078
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.000079
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylpropanamide
0.0001
-
 inhibition of erbB2 in a mouse BT474C xenograft model Homo sapiens (2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.00012
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N-(2-methoxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.00012
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N-(2-hydroxyethyl)-N-methylacetamide
0.00013
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]acetamide
0.00014
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-(2-morpholin-4-yl-2-oxoethoxy)quinazolin-4-amine
0.00018
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]acetamide
0.0002
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N-(2-hydroxyethyl)-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.00027
-
 inhibition of erbB2 in a mouse BT474C xenograft model Homo sapiens (2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.00032
-
 inhibition of erbB2 in a mouse BT474C xenograft model Homo sapiens (2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.00035
-
 inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]-5-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]quinazolin-4-amine
0.001
-
 inhibition of erbB2 in KB cells Homo sapiens (2R)-2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.0027
-
 inhibition of erbB2 in KB cells Homo sapiens (2R)-N,N-dimethyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide
0.023
-
 inhibition of erbB2 in KB cells Homo sapiens (2R)-N-(2-hydroxyethyl)-N-methyl-2-[[4-([3-methyl-4-[(6-methylpyridin-3-yl)oxy]phenyl]amino)quinazolin-5-yl]oxy]propanamide