diminazene [Ligand Id: 10307] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL35241 (4,4'-(diazoamino)benzamidine, Diminazen, Diminazene)
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Spermidine/spermine N(1)-acetyltransferase 1 in Human [ChEMBL: CHEMBL4286] [UniProtKB: P21673]
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  • ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
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  • ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
GtoPdb - - 6.5 pIC50 - - - Br J Pharmacol (2018) 175: 2204-2218 [PMID:29134638];
PLoS One (2018) 13: e0196894 [PMID:29782492];
Mol Pharmacol (2017) 92: 665-675 [PMID:29025967]
ASIC1/Acid-sensing ion channel 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3232694] [GtoPdb: 684] [UniProtKB: Q6NXK8]
ChEMBL Inhibition of pH 6.6-stimulated mouse ASIC1a homomer expressed in CHOK1 cells assessed as reduction in channel activation by VSD fluorescence assay B 4.24 pIC50 56900 nM IC50 ACS Med Chem Lett (2019) 10: 627-632 [PMID:30996808]
cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858]
ChEMBL Inhibition of human liver cathepsin B B 4.52 pIC50 >30000 nM IC50 J Med Chem (2008) 51: 545-552 [PMID:18173229]
Diamine oxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2118] [UniProtKB: P19801]
ChEMBL Mixed type inhibition of recombinant human DAO expressed in drosophila S2 cells B 7.89 pKi 13 nM Ki Bioorg Med Chem (2014) 22: 1983-1992 [PMID:24630693]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake F 6.72 pIC50 190 nM IC50 Eur J Med Chem (2008) 43: 2840-2852 [PMID:18395298]
Spermidine/spermine N(1)-acetyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4286] [UniProtKB: P21673]
ChEMBL Inhibition of human SSAT using spermidine as substrate B 5.62 pKi 2400 nM Ki Bioorg Med Chem (2014) 22: 1983-1992 [PMID:24630693]
ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
GtoPdb - - 6.1 pIC50 - - - Br J Pharmacol (2018) 175: 2204-2218 [PMID:29134638]
ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
GtoPdb - - 6.5 pIC50 - - - Br J Pharmacol (2018) 175: 2204-2218 [PMID:29134638]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]