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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:Q6ZXD5_BOVIN
Synonyms:
Inducible nitric oxid synthase
EC-Numbers:1.14.13.39
Organism:Bos taurus
Bovine
PDB IDs:-

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.