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Literature summary for 2.7.10.1 extracted from

  • Hanan, E.; Baumgardner, M.; Bryan, M.; Chen, Y.; Eigenbrot, C.; Fan, P.; Gu, X.; La, H.; Malek, S.; Purkey, H.; Schaefer, G.; Schmidt, S.; Sideris, S.; Yen, I.; Yu, C.; Heffron, T.
    4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase (2016), Bioorg. Med. Chem. Lett., 26, 534-539.
    View publication on PubMed
Search for more literature for 2.7.10.1

Inhibitors

Inhibitors Comment Organism Structure
4-(1H-indazol-3-yloxy)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidine
-
 Homo sapiens
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-(4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[6-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[7-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
7,7-dimethyl-N-(1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
7,7-dimethyl-N-(5-methyl-1H-pyrazol-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1,2-benzothiazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1,3-benzothiazol-2-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1,3-thiazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1-methyl-1H-pyrazol-5-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-1,2,3-triazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indazol-3-yl)-N,7,7-trimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(1H-indol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(4,5-dichloro-1H-pyrazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(4-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(5,7-difluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(6-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-chloro-5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-chloro-6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-fluoro-1-methyl-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
N-(7-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine
-
 Homo sapiens
[7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl](1H-indazol-3-yl)methanone
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a [protein]-L-tyrosine Homo sapiens
-
 ADP + a [protein]-L-tyrosine phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
non-small cell lung cancer cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a [protein]-L-tyrosine
-
 Homo sapiens ADP + a [protein]-L-tyrosine phosphate
-
 ?

Synonyms

Synonyms Comment Organism
Egfr
-
 Homo sapiens
epidermal growth factor receptor tyrosine kinase
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000002
-
 N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000002
-
 N-(6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000002
-
 N-(7-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000003
-
 N-(7-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000004
-
 N-(7-chloro-6-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000005
-
 N-(5,7-difluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.0000056
-
 N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1,3-thiazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000008
-
 N-(5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000009
-
 N-(7-chloro-1H-indazol-3-yl)-2-[5-(difluoromethyl)-1H-pyrazol-4-yl]-7,7-dimethyl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000016
-
 N-(6-chloro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000016
-
 N-(7-chloro-5-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000017
-
 N-(1H-indol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000017
-
 N-(4-fluoro-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.0000343
-
 N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1-methyl-1H-pyrazol-5-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000057
-
 N-(7-fluoro-1-methyl-1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000085
-
 4-(1H-indazol-3-yloxy)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidine pH and temperature not specified in the publication Homo sapiens
0.000104
-
 [7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-yl](1H-indazol-3-yl)methanone pH and temperature not specified in the publication Homo sapiens
0.000134
-
 7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[7-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000175
-
 N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000389
-
 N-(4,5-dichloro-1H-pyrazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000519
-
 N-(1H-indazol-3-yl)-N,7,7-trimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000732
-
 N-(1H-indazol-3-yl)-7,7-dimethyl-2-(1H-1,2,3-triazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000747
-
 N-(1,2-benzothiazol-3-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.000844
-
 7,7-dimethyl-N-(5-methyl-1H-pyrazol-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.002
-
 7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-(4,5,6,7-tetrahydro-1H-indazol-3-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.002
-
 N-(1,3-benzothiazol-2-yl)-7,7-dimethyl-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.002
-
 7,7-dimethyl-N-(1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(1H-pyrazol-4-yl)-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens
0.002
-
 7,7-dimethyl-2-(1H-pyrazol-4-yl)-N-[6-(trifluoromethyl)-1H-indazol-3-yl]-5,7-dihydrofuro[3,4-d]pyrimidin-4-amine pH and temperature not specified in the publication Homo sapiens