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Drug-Target Interaction

Drug

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PubChem ID:795
Structure:
Synonyms:
1,3-Diaza-2,4-cyclopentadiene
1,3-Diaza-2,4-cyclopentadiene-
1,3-Diazole
116421-26-2
146117-15-9
1467-16-9
1467-16-9 (mono-hydrochloride)
1H-Imidazole
1H-Imidazole (9CI)
288-32-4
4286D518-643C-4C69-BCE7-519D073F4992
5-23-04-00191 (Beilstein Handbook Reference)
5587-42-8
5587-42-8 (hydrochloride salt)
56748_FLUKA
56748_SIGMA
56749_FLUKA
56749_SIGMA
56750_FLUKA
56750_SIAL
68268_FLUKA
68268_SIGMA
AB1002136
AC1L1A1H
AC1Q4W12
AC1Q4W13
AG-E-93194
AI3-24703
AIDS-008702
AIDS008702
AKOS000120177
BB_SC-6938
bmse000096
BRN 0103853
C01589
C3H4N2
CCRIS 3345
CHEBI:16069
CHEMBL540
EINECS 206-019-2
Formamidine, N,N'-vinylene-
Glioksal
Glioksal [Polish]
Glyoxalin
Glyoxaline
Glyoxaline solution
Him
I0001
I0014
I0125_SIGMA
I0250_SIGMA
I0288
I0290
I14-0665
I14-10573
I2399_SIAL
I5513_SIGMA
IMD
Imidazol
imidazole
Imidazole (8CI)
Imidazole buffer Solution
Imidazole solution
IMIDAZOLE-RING
Iminazole
Imutex
LS-77964
Methanimidamide, N,N'-1,2-ethenediyl-
Miazole
MLS001055465
MolPort-000-156-418
N,N'-1,2-ethenediylmethanimidamide
N,N'-vinyleneformamidine
NCGC00090984-01
NCGC00090984-02
nchem.892-comp5
NCIStruc1_001975
NCIStruc2_000693
NSC 51860
NSC 60522
NSC51860
NSC60522
Pyrro(b)monazole
Pyrro[b]monazole
SMR000057825
ST097249
ST5214389
STK362967
TL8002274
Unavailable - See ASDI_CatNo 500012277
Usaf ek-4733
WLN: T5M CNJ
ZINC00901039

Target

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Uniprot ID:NOS3_BOVIN
Synonyms:
cNOS
Constitutive NOS
EC-NOS
Endothelial NOS
eNOS
Nitric oxide synthase, endothelial
NOS type III
NOSIII
EC-Numbers:1.14.13.39
Organism:Bos taurus
Bovine
PDB IDs:1D0C 1D0O 1D1V 1D1W 1D1X 1D1Y 1DM6 1DM7 1DM8 1DMI 1DMJ 1DMK 1ED4 1ED5 1ED6 1FOI 1FOJ 1FOL 1FOO 1FOP 1I83 1NSE 1P6L 1P6M 1P6N 1Q2O 1RS8 1RS9 1ZZS 1ZZT 2G6O 2HX2 2NSE 3DQS 3DQT 3E7S 3NSE 4NSE 5NSE 6NSE 7NSE 8NSE 9NSE
Structure:
9NSE

Binding Affinities:

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

References:

7526799
The inhibition of the constitutive bovine endothelial nitric oxide synthase by imidazole and indazole agents.. D J Wolff; A Lubeskie; S Umansky (1994) Archives of biochemistry and biophysics display abstract
Citrulline formation by the Ca2+ CaM-dependent nitric oxide synthase of bovine endothelium is inhibited reversibly by 7-nitroindazole, 1-phenylimidazole, and imidazole. As measured at 0.67 microM (6R)-5,6,7,8-tetrahydrobiopterin (BH4), IC50 values of 0.8, 200, and 50 microM were determined for 7-nitroindazole, 1-phenylimidazole, and imidazole, respectively. Increasing concentrations of added BH4 cofactor increased the IC50 values for 7-nitroindazole and 1-phenylimidazole but did not alter the IC50 value for imidazole. 7-nitroindazole inhibited citrulline formation by the endothelial cNOS noncompetitively versus arginine substrate but competitively versus BH4 with a Ki value of 0.8 microM. 1-Phenylimidazole inhibited citrulline formation by the endothelial cNOS competitively versus both arginine substrate and BH4 with a Ki value of 50 microM. Imidazole inhibited citrulline formation competitively versus arginine substrate but noncompetitively versus BH4 with a Ki value of 50 microM. Neither 7-nitroindazole, 1-phenylimidazole, nor imidazole inhibited the cytochrome c reductase activity of endothelial cNOS at concentrations up to 5000-fold higher than their Ki values for inhibition of citrulline formation. By comparison with the previously determined kinetic properties of the other nitric oxide synthase isoforms, these observations establish that 1-phenylimidazole displays marked specificity for inhibiting the inducible nitric oxide synthase isoform and, since 7-nitroindazole has been reported not to elevate blood pressure (McCall et al., 1991, Br. J. Pharmacol. 102, 234-238), fails to confirm the expected insensitivity of the constitutive endothelial nitric oxide synthase to inhibition by 7-nitroindazole.