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Drug-Target Interaction

Drug

show drug details
PubChem ID:123631
Structure:
Synonyms:
"gefitini; iressa"
184475-35-2
4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazolin
4-(3'-Chloro-4'-fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy)quinazoline
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-
4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-4-morpholin)propoxy)-
6-(3-morpholinopropoxy)-N-(3-chloro-4-fluorophenyl)-7-methoxyquinazolin-4-amine
BCB03_000781
C419708
CCRIS 9011
CHEBI:49668
CU-00000000396-1
D01977
DB00317
Gefitini; Iressa
Gefitinib
Gefitinib (JAN/USAN/INN)
Gefitinib [USAN]
IRE
Iressa
Iressa (TN)
Irressat
K00240
KBioSS_002241
LS-139916
N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamide
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-(4-morpholinyl)propoxy)-4-quinazolinamine
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine
NCGC00159455-02
NCGC00159455-03
nchembio.117-comp18
nchembio866-comp14
NSC715055
STOCK6S-52331
ZD 1839
ZD-1839
ZD-1839, Iressa, Gefitinib
ZD1839
ZINC19632614
ATC-Codes:
Side-Effects:
Side-EffectFrequency
rash0.21499999
diarrhea0.19199999
acne0.125
dry skin0.065
nausea0.051999997
vomiting0.048
pruritus0.04
anorexia0.035
asthenia0.03
interstitial lung disease0.0010
toxic epidermal necrolysis0.0010
allergic reactions0.0010
eye pain0.0010
idiopathic pulmonary fibrosis0.0010
ulcer0.0010
interstitial pneumonia0.0010
pneumonitis0.0010
pancreatitis0.0010
cough0.0010
dyspnea0.0010
epistaxis0.0010
erythema multiforme0.0010
angioedema and urticaria0.0010
fever0.0010
hematuria0.0010
haemorrhage0.0010
ischemia0.0010
deep thrombophlebitis0
bundle branch block0
dry eyes0
mouth ulceration0
gastrointestinal hemorrhage0
peripheral edema0
exfoliative dermatitis0
dermatitis0
hypotension0
constitutional symptoms0
hemoptysis0
electrolyte imbalance0
tumor0
melena0
infection0
shock0
pleural effusion0
hypokalemia0
fatigue0
respiratory failure0
heart disease0
hypoxia0
conjunctivitis0
arrhythmia0
hypomagnesemia0
mediastinal disorders0
stevens - johnson syndrome0
thrombocytopenia0
stomatitis0
amblyopia0
sgot increased0
seborrhea0
constipation0
paronychia0
alopecia0
pain0
neutropenia0
nail disorder0
anemia0
dry mouth0
blepharitis0
urticaria0
abdominal pain0
dehydration0
atrial fibrillation0
pneumoconiosis0
edema0
vascular disorders0
weight loss0

Target

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Uniprot ID:POKL_HUMAN
Synonyms:
Putative HERV-K_Xq28 provirus ancestral Pol protein
EC-Numbers:2.7.7.49
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

17094457
Antiproliferative effects of gefitinib are associated with suppression of E2F-1 expression and telomerase activity.. Mitsuhiro Suenaga; Akihiko Yamaguchi; Hiroshi Soda; Koji Orihara; Yuichi Tokito; Yoshimune Sakaki; Megumi Umehara; Kenji Terashi; Nakaaki Kawamata; Mikio Oka; Shigeru Kohno; Chuwa Tei (2006) Anticancer research display abstract
BACKGROUND: Gefitinib (Iressa, ZD1839) is a selective epidermal growth factor receptor tyrosine kinase inhibitor. E2F-1 is a critical determinant in cell cycle. Growth signals up-regulate telomerase activity. The effects of gefitinib on E2F-1 and telomerase in A549, H23 and A431 cells were examined. MATERIALS AND METHODS: Cell proliferation and cell cycle progression were measured by the WST-1 assay and flow cytometry. The expression of E2F-1 and cyclin-dependent kinase inhibitors was evaluated, and hTERT mRNA expression and telomerase activity were analyzed. RESULTS: In the A431 and A549 cells, treatment with gefitinib inhibited cell proliferation and was associated with an increase in G1-phase. In both cell types, gefitinib decreased the expression of E2F-1 mRNA and protein, followed by the suppression of hTERT mRNA and telomerase activity. In the H23 cells, gefitinib did not affect cell proliferation. CONCLUSION: The antiproliferative effects of gefitinib may be, at least in part, due to the inhibition of E2F-1 expression and telomerase activity.