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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]