aminoguanidine [Ligand Id: 5135] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL225304 (Aminoguanidine, Pimagedine)
  • aldo-keto reductase family 1 member B/Aldose reductase in Rat [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
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  • Neuronal NOS/Nitric-oxide synthase, brain in Human [ChEMBL: CHEMBL3568] [GtoPdb: 1251] [UniProtKB: P29475]
  • Neuronal NOS/Nitric-oxide synthase, brain in Rat [ChEMBL: CHEMBL3048] [GtoPdb: 1251] [UniProtKB: P29476]
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  • Endothelial NOS/Nitric-oxide synthase, endothelial in Human [ChEMBL: CHEMBL4803] [GtoPdb: 1249] [UniProtKB: P29474]
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  • Inducible NOS/Nitric oxide synthase, inducible in Human [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
ChEMBL Inhibition of Sprague-Dawley rat lens aldose reductase B 4.52 pIC50 >30000 nM IC50 J. Nat. Prod. (2012) 75: 267-270 [PMID:22264115]
Diamine oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2118] [UniProtKB: P19801]
ChEMBL Tested for ability to competitively inhibit hog kidney diamine oxidase (DAO) in a spectrometric assay B 6.85 pKi 140 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 353-356
Neuronal NOS/Nitric-oxide synthase, brain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3568] [GtoPdb: 1251] [UniProtKB: P29475]
ChEMBL Inhibition of nNOS assessed as conversion of L-[3H]arginine to L-[3H]citrulline B 5.48 pKi 3300 nM Ki Bioorg. Med. Chem. (2008) 16: 6193-6206 [PMID:18477512]
ChEMBL Inhibitory activity against human neuronal nitric oxide synthase B 5.23 pIC50 5900 nM IC50 J. Med. Chem. (2003) 46: 913-916 [PMID:12620067]
Neuronal NOS/Nitric-oxide synthase, brain in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3048] [GtoPdb: 1251] [UniProtKB: P29476]
ChEMBL Inhibition of nNOS in Sprague-Dawley rat brain homogenates assessed as conversion of oxyhemoglobin to methemoglobin measured for 10 mins by UV-visible spectrophotometer analysis B 4.71 pIC50 19410 nM IC50 Bioorg. Med. Chem. (2011) 19: 3935-3944 [PMID:21665485]
ChEMBL Inhibition of conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by neuronal NOS (n NOS) from rat cerebellum F 5.22 pIC50 6000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 1023-1026 [PMID:11327580]
Endothelial NOS/Nitric-oxide synthase, endothelial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4803] [GtoPdb: 1249] [UniProtKB: P29474]
ChEMBL Inhibitory activity against human endothelial nitric oxide synthase B 4 pIC50 100000 nM IC50 J. Med. Chem. (2003) 46: 913-916 [PMID:12620067]
ChEMBL Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by endothelial NOS (e NOS) from HUVEC cells F 4.14 pIC50 72000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 1023-1026 [PMID:11327580]
Inducible NOS/Nitric oxide synthase, inducible in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
ChEMBL Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from human DLD-1 cells. B 4.27 pIC50 54000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1573-1576
ChEMBL Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by inducible NOS (i NOS) from human DLD-1 cells F 5.35 pIC50 4500 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 1023-1026 [PMID:11327580]
ChEMBL Inhibitory activity of compound against human inducible nitric oxide synthase B 5.41 pIC50 3900 nM IC50 J. Med. Chem. (2003) 46: 913-916 [PMID:12620067]
Inducible NOS/Nitric oxide synthase, inducible in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
ChEMBL Inhibition of iNOS-mediated NO production in LPS-stimulated mouse RAW264.7 cells after 24 hrs by Griess reagent method B 4.55 pIC50 28470 nM IC50 J. Nat. Prod. (2011) 74: 2489-2496 [PMID:22148193]
ChEMBL Inhibition of iNOS in mouse RAW264.7 cells assessed as anti-inflammatory activity by measuring maximum inhibition of LPS-induced nitric oxide production after 24 hrs B 4.58 pIC50 26550 nM IC50 J. Nat. Prod. (2011) 74: 1875-1880 [PMID:21846089]
ChEMBL Tested to inhibit the conversion of [3H]L-arginine to [3H]L-citrulline catalyzed by inducible NOS from mouse macrophage J774 cells B 5.05 pIC50 9000 nM IC50 Bioorg. Med. Chem. Lett. (1995) 5: 1573-1576

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]