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Literature summary for 2.7.10.1 extracted from

  • Gangjee, A.; Zaware, N.; Raghavan, S.; Yang, J.; Thorpe, J.; Ihnat, M.
    N4-(3-bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: Design, synthesis, and in vivo evaluation (2012), Bioorg. Med. Chem., 20, 2444-2454.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.1

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking studies using inhibitor N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine. The compound binds to the ATP binding site of platelet derived growth factor receptor-beta with the pyrrolo[2,3-d]pyrimidine portion occupying the adenine binding site Homo sapiens
molecular docking studies using inhibitor N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine. The pyrrolo[2,3-d]pyrimidine ring occupies the adenine binding portion of the ATP binding site. The 2-NH2 moiety is involved in a hydrogen bond with Glu915 in the Hinge region while the N3 and 4-anilino NH are involved in hydrogen bonds with the backbone of Cys917 in the Hinge region. Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2; dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2 Homo sapiens
N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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 Homo sapiens
N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2. In a COLO-205, in vivo tumor mouse model, compound demonstrates inhibition of tumor growth, metastasis, and tumor angiogenesis; dual inhibitor of platelet derived growth factor recptor-beta and vascular endothelial growth factor receptor 2. In a COLO-205, in vivo tumor mouse model, compound demonstrates inhibition of tumor growth, metastasis, and tumor angiogenesis Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09619
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Homo sapiens P35968
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Source Tissue

Source Tissue Comment Organism Textmining
A-431 cell
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 Homo sapiens
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OVCAR-8 cell
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 Homo sapiens
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SF-539 cell
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 Homo sapiens
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Synonyms

Synonyms Comment Organism
PDGFRB
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 Homo sapiens
PDGFRbeta
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 Homo sapiens
platelet derived growth factor receptor-beta
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 Homo sapiens
vascular endothelial growth factor receptor 2
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 Homo sapiens
VEGFR-2
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 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0015
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0018
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0149
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0179
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromophenyl)-7-(2-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.0257
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromo-phenyl)-7-(3,4,5-trimethoxy-benzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
0.129
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N4-(3-bromophenyl)-7-(1-naphthylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine