Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.10.1 extracted from

  • Usui, T.; Ban, H.S.; Kawada, J.; Hirokawa, T.; Nakamura, H.
    Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening (2008), Bioorg. Med. Chem. Lett., 18, 285-288.
    View publication on PubMed
Search for more literature for 2.7.10.1

Application

Application Comment Organism
drug development series of indenopyrazoles designed and synthesized as EGFR tyrosine kinase inhibitors by in silico highthroughput screening Homo sapiens
drug development series of indenopyrazoles designed and synthesized as KDR inhibitors by in silico highthroughput screening Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
EGFR tyrosine kinase domain in complex with erlotinib Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4-aminophenyl)-3-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea 61% inhibition of EGFR; 88% inhibition of KDR Homo sapiens
1-(4-aminophenyl)-3-[3-(3,4-dihydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea 50% inhibition of EGFR; 58% inhibition of KDR Homo sapiens
1-(4-aminophenyl)-3-[3-(4-hydroxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea 65% inhibition of EGFR; 73% inhibition of KDR Homo sapiens
1-(4-aminophenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea 3% inhibition of EGFR; 42% inhibition of KDR Homo sapiens
1-(4-hydroxyphenyl)-3-[3-(4-methoxyphenyl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]urea 44% inhibition of KDR; 7% inhibition of EGFR Homo sapiens
1-[3-(1,3-benzodioxol-5-yl)-4-oxo-2,4-dihydroindeno[1,2-c]pyrazol-5-yl]-3-(4-hydroxyphenyl)urea 4% inhibition of EGFR; 70% inhibition of KDR Homo sapiens
AAL 993 30% inhibition of EGFR; 95% inhibition of KDR Homo sapiens
erlotinib
-
 Homo sapiens
Tarceva 38% inhibition of KDR; 81% inhibition of EGFR Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00533
-
-
Homo sapiens P35968
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-431 cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
EGFR tyrosine kinase
-
 Homo sapiens
erb-B1
-
 Homo sapiens
HER-1
-
 Homo sapiens
KDR
-
 Homo sapiens
VEGFR-2 tyrosine kinase
-
 Homo sapiens