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Drug-Target Interaction

Drug

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PubChem ID:3899
Structure:
Synonyms:
(5-methylisoxazol-4-yl)-N-[4-(trifluoromethyl)phenyl]carboxamide
210165-51-8
4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl
4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl)-
4-isoxazolecarboxamide,5-methyl-N-(4-(trifluoromethyl)phenyl)
5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide
5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide
5-methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
5-methyl-N-[4-(trifluoromethyl)phenyl]isoxazole-4-carboxamide
5-Methylisoxazole-4-(4-trifluoromethyl)carboxanilide
5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide)
5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide
75706-12-6
A77 1486
AB00052389
AC-6796
AC1L1GYK
AC1Q2EVA
AIDS-009747
AIDS009747
AKOS000265193
alpha,alpha,alpha-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide
AP-501/42475599
Arava
Arava (TN)
Arava, Leflunomide
Aventis Behring Brand of Leflunomide
Aventis Brand of Leflunomide
Aventis Pharma Brand of Leflunomide
BIDD:PXR0189
BPBio1_000930
BRD-K78692225-001-03-9
BSPBio_000844
C045463
C07905
C12H9F3N2O2
CAS-75706-12-6
CCG-204736
CHEBI:6402
CHEMBL960
D00749
DB01097
DivK1c_000916
EU-0100649
HMS1570K06
HMS1922M06
HMS2090O12
HMS2097K06
HMS2235C07
HMS3262A19
HMS502N18
Hoechst Brand of Leflunomide
HSDB 7289
HWA 486
HWA-486
I06-2131
IDI1_000916
Isoxazole-4-carboxamide, 5-methyl-N-[4-(trifluoromethyl)phenyl]-
KBio1_000916
KBio2_000802
KBio2_003370
KBio2_005938
KBioSS_000802
KS-1076
L 5025
L5025_SIGMA
Leflunomid
Leflunomida
Leflunomida [INN-Spanish]
Leflunomide
Leflunomide (JAN/USAN/INN)
Leflunomide [USAN:INN]
Leflunomide-Supplied by Selleck Chemicals
Leflunomidum
Leflunomidum [INN-Latin]
LEFUNAMIDE
Lefunomide [Inn-Spanish]
Lopac-L-5025
Lopac0_000649
LS-86580
MLS-0003109.0001
MLS000069648
MLS001076267
N-(4'-Trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide
N-(4-trifluoromethyphenyl)-5-methylisoxazole-4-carboxamide
NCGC00015610-01
NCGC00015610-02
NCGC00015610-03
NCGC00015610-04
NCGC00015610-05
NCGC00015610-06
NCGC00015610-07
NCGC00015610-08
NCGC00015610-09
NCGC00015610-10
NCGC00015610-11
NCGC00015610-12
NCGC00015610-13
NCGC00015610-14
NCGC00022625-03
NCGC00022625-04
NCGC00022625-05
NCGC00022625-06
NCGC00022625-07
NCGC00022625-08
NINDS_000916
NSC677411
Prestwick0_000772
Prestwick1_000772
Prestwick2_000772
Prestwick3_000772
Prestwick_87
Repso
RS-34821
S1247_Selleck
SMR000058209
SPBio_002783
SPECTRUM1503927
Spectrum5_000850
Spectrum_000322
ST079287
SU 101
SU 101 (pharmaceutical)
SU-101
SU101
TL8005179
UNII-G162GK9U4W
ZINC00004840
ATC-Codes:
Side-Effects:
Side-EffectFrequency
diarrhea0.16056518
nausea0.12331707
infection0.1161396
headache0.10737254
dyspepsia0.085952364
rash0.08320927
alopecia0.07594736
back pain0.061333306
bronchitis0.054374997
abdominal pain0.051911104
mouth ulcer0.04910526
cough0.048235282
urinary tract infection0.043437496
dizziness0.04331579
asthenia0.042827576
joint disorder0.042214278
pruritus0.03837837
sinusitis0.038108107
hypertension0.037079357
rhinitis0.034999996
anorexia0.03333333
flu syndrome0.0325
vomiting0.032199997
arthralgia0.031499997
pain0.030564098
leg cramps0.028108107
chest pain0.025238097
gastroenteritis0.024999997
allergic reaction0.023891302
paresthesia0.02344827
tenosynovitis0.022142855
eczema0.018571429
pharyngitis0.018538462
hypokalemia0.017619047
weight loss0.01563636
dry skin0.015517242
pneumonia0.015000001
synovitis0.0146875
tachycardia0.0010
stevens - johnson syndrome0.0010
stomatitis0.0010
aphthous stomatitis0.0010
upper respiratory tract infections0.0010
tooth disorder0.0010
thrombocytopenia0.0010
amblyopia0.0010
skin ulcer0.0010
skin nodule0.0010
palpitation0.0010
pancreatitis0.0010
pancytopenia0.0010
angioedema0.0010
pelvic pain0.0010
peripheral neuropathy0.0010
angina pectoris0.0010
pulmonary fibrosis0.0010
anemia0.0010
anaphylactic reaction0.0010
anxiety0.0010
albuminuria0.0010
urticaria0.0010
interstitial pneumonitis0.0010
interstitial lung disease0.0010
malaise0.0010
myalgia0.0010
sepsis0.0010
lymphadenopathy0.0010
juvenile rheumatoid arthritis0.0010
urinary frequency0.0010
acne0.0010
sleep disorder0.0010
insomnia0.0010
iron deficiency anemia0.0010
bone pain0.0010
varicose vein0.0010
vasculitis0.0010
vertigo0.0010
agranulocytosis0.0010
dry mouth0.0010
hepatic failure0.0010
peripheral edema0.0010
cataract0.0010
abscess0.0010
migraine0.0010
gingivitis0.0010
hepatic necrosis0.0010
bone necrosis0.0010
cyst0.0010
epistaxis0.0010
erythema multiforme0.0010
esophagitis0.0010
connective tissue disorders0.0010
fever0.0010
flatulence0.0010
gastritis0.0010
conjunctivitis0.0010
colitis0.0010
cholelithiasis0.0010
hematoma0.0010
toxic epidermal necrolysis0.0010
eosinophilia0.0010
contact dermatitis0.0010
fungal dermatitis0.0010
diabetes mellitus0.0010
cystitis0.0010
bursitis0.0010
abuse0.0010
constipation0.0010
dyspnea0.0010
dysuria0.0010
ecchymosis0.0010
endocrine disorders0.0010
hematuria0.0010
hepatitis0.0010
hernia0.0010
nodule0.0010
lung disorder0.0010
mediastinal disorders0.0010
melena0.0010
menstrual disorder0.0010
muscle cramps0.0010
nail disorder0.0010
asthma0.0010
neuralgia0.0010
neuritis0.0010
neutropenia0.0010
leucopenia0.0010
breast disorders0.0010
malignancy0.0010
herpes simplex0.0010
herpes zoster0.0010
hyperglycemia0.0010
hyperlipidemia0.0010
hypersensitivity0.0010
neck pain0.0010
hyperthyroidism0.0010
vaginal moniliasis0.0010
oral moniliasis0.0010
jaundice0.0010
blurred vision0
elevated liver enzymes0
increased sweating0
liver function tests abnormal0
liver disease0

Target

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Uniprot ID:NOS2_HUMAN
Synonyms:
HEP-NOS
Hepatocyte NOS
Inducible NO synthase
Inducible NOS
iNOS
Nitric oxide synthase, inducible
NOS type II
EC-Numbers:1.14.13.39
Organism:Homo sapiens
Human
PDB IDs:1NSI 2NSI 3E7G 3EJ8 3HR4 4NOS
Structure:
4NOS

Binding Affinities:

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

References:

8680047
Molecular mechanisms of new immunosuppressants.. P F Halloran (1996) Clinical transplantation display abstract
Maintenance immunosuppressive drugs act by partially blocking rate-limiting steps in the immune response. The new maintenance immunosuppressive drugs are either inhibitors of de novo synthesis of nucleotides (purines or pyrimidines), or are immunophilin-binding drugs that inhibit signal transduction in lymphocytes. The new inhibitors of de novo nucleotide synthesis include mycophenolate mofetil (MMF), mizoribine (MZ), brequinar (BQR), and leflunomide (LEF). MMF and MZ act to inhibit de novo purine synthesis, by inhibition of inosine monophosphate dehydrogenase (IMPDH). They create a selective immunodeficiency in T and B lymphocytes. MMF is hydrolyzed to mycophenolic acid (MPA), an uncompetitive inhibitor of IMPDH. MPA reduces the pools of guanine nucleotides, and increases some adenine nucleotides, inhibiting the cell cycle. Thus the number of specific effector T and B lymphocytes is reduced by limiting clonal expansion. MZ is a competitive inhibitor of IMPDH, which creates a similar defect. The relative clinical effectiveness of MMF versus MZ is not known. MMF has been approved in a number of countries; MZ has been approved in Japan. The inhibitors of de novo pyrimidine synthesis (BQR, LEF) act on the enzyme dehydroorotate dehydrogenase. Neither is currently in clinical trials in transplantation. The new immunophilin-binding drugs inhibit either the calcium-dependent phosphatase calcineurin (CN) [tacrolimus (or FK-506) and the microemulsion form of cyclosporine (CsA)] or signaling from growth factor receptors [rapamycin (sirolimus)]. Tacrolimus binds to FK binding protein-12 (FKBP-12) to create a complex that inhibits CN. CsA binds to cyclophilin to create a complex that inhibits CN. Inhibition of CN prevents activation of cytokine genes in T cells. The relative clinic effectiveness of tacrolimus versus microemulsion CsA is unknown. Rapamycin inhibits signaling from growth factor receptors, such as IL-2R. Rapamycin binds to FKBP to create a complex that engages proteins called TOR (target of rapamycin), or RAFT (rapamycin and FKBP target), which may be kinases. The result is a block in the ability of cytokine receptors to activate cell cycling, interfering with clonal expression. Deoxyspergualin, a parenteral drug in development for induction or antirejection therapy, may inhibit intracellular chaperoning by Hsc70, a member of the heat shock protein family. It may have its principal effect by inhibiting the activation of transcription factor NF-kappa B in antigen-presenting cells and monocytes.