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Literature summary for 2.7.10.1 extracted from

  • Barlaam, B.; Acton, D.G.; Ballard, P.; Bradbury, R.H.; Cross, D.; Ducray, R.; Germain, H.; Hudson, K.; Klinowska, T.; Magnien, F.; Ogilvie, D.J.; Olivier, A.; Ross, H.S.; Smith, R.; Trigwell, C.B.; Vautier, M.; Wright, L.
    Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of ErbB2 receptor tyrosine kinase (2008), Bioorg. Med. Chem. Lett., 18, 1799-1803.
    View publication on PubMed

Application

Application Comment Organism
drug development new series of C-5 substituted indazolylaminoquinazolines as potent ErbB2 kinase inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
Homo sapiens
(2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
-
Homo sapiens
(2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
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-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
-
Homo sapiens
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
(2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
-
Homo sapiens
5-(2-morpholin-4-yl-2-oxoethoxy)-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1R)-1-methyl-2-oxo-2-pyrrolidin-1-ylethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
-
Homo sapiens
N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]acetamide
-
Homo sapiens
N-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]quinazolin-4-amine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P04626
-
-

Source Tissue

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

Synonyms

Synonyms Comment Organism
erbB2 receptor tyrosine kinase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000027
-
5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine inhibition versus erbB2 kinase Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.000008
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N,N-dimethylpropanamide
0.000008
-
inhibition versus erbB2 kinase Homo sapiens (2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.000012
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
0.000022
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens N-[1-(3-fluorobenzyl)-1H-indazol-5-yl]-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
0.000024
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.000026
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.000032
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.000043
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
0.000051
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
0.000057
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]-N-methylpropanamide
0.000059
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N-methyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00008
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00009
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N,N-dimethyl-2-[(4-[[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00013
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2S)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00014
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00014
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 5-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
0.00016
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens 5-[(1R)-1-methyl-2-morpholin-4-yl-2-oxoethoxy]-N-[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]quinazolin-4-amine
0.00023
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N,N-dimethyl-2-[(4-[[1-(1,3-thiazol-4-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide
0.00024
-
inhibition versus erbB2 cellular autophosphorylation in MCF-7 cells Homo sapiens (2R)-N-methyl-2-[(4-[[1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-yl]amino]quinazolin-5-yl)oxy]propanamide