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Literature summary for 2.7.10.1 extracted from

  • Ballard, P.; Barlaam, B.C.; Bradbury, R.H.; Dishington, A.; Hennequin, L.F.; Hickinson, D.M.; Hollingsworth, I.M.; Kettle, J.G.; Klinowska, T.; Ogilvie, D.J.; Pearson, S.E.; Scott, J.S.; Suleman, A.; Whittaker, R.; Williams, E.J.; Wood, R.; Wright, L.
    Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase (2007), Bioorg. Med. Chem. Lett., 17, 6326-6329.
    View publication on PubMed
Search for more literature for 2.7.10.1

Inhibitors

Inhibitors Comment Organism Structure
(R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol IC50: 97 nM; IC50: less than 2 nM Mus musculus
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide IC50: 3 nM; IC50: less than 2 nM Mus musculus
(R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide IC50: 2 nM; IC50: less than 2 nM Mus musculus
(S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol IC50: 2 nM; IC50: 327 nM Mus musculus
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide IC50: 19 nM; IC50: 2580 nM Mus musculus
(S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide IC50: 191 nM; IC50: 22 nM Mus musculus
N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide IC50: 35 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole; IC50: 4 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Synonyms

Synonyms Comment Organism
Egfr
-
 Mus musculus
erbB2 receptor tyrosine kinase
-
 Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
 IC50: 2 nM Mus musculus (R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000002
-
 IC50: 2 nM Mus musculus (S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000002
-
 IC50: less than 2 nM Mus musculus (R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000002
-
 IC50: less than 2 nM Mus musculus (R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000002
-
 IC50: less than 2 nM Mus musculus (R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000003
-
 IC50: 3 nM Mus musculus (R)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000004
-
 IC50: 4 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole Mus musculus N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
0.000019
-
 IC50: 19 nM Mus musculus (S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide
0.000022
-
 IC50: 22 nM Mus musculus (S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000035
-
 IC50: 35 nM, potent, orally active inhibitor when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole Mus musculus N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]ethyl]-2-hydroxyacetamide
0.000097
-
 IC50: 97 nM Mus musculus (R)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.000191
-
 IC50: 191 nM Mus musculus (S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]propyl]-2-hydroxyacetamide
0.000327
-
 IC50: 327 nM Mus musculus (S)-2-(2-[[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]methyl]pyrrolidin-1-yl)-2-oxoethanol
0.00258
-
 IC50: 2580 nM Mus musculus (S)-N-[2-[(4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]quinazolin-5-yl)oxy]-1-methylethyl]-2-hydroxyacetamide