Application | Comment | Organism |
---|---|---|
drug development | new series of C-5 substituted indazolylaminoquinazolines as potent ErbB2 kinase inhibitors | Homo sapiens |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P04626 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
MCF-7 cell | - |
Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
erbB2 receptor tyrosine kinase | - |
Homo sapiens |
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 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 |