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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL35241 (4,4'-(diazoamino)benzamidine, Diminazen, Diminazene, Diminazeno)
Created with Highcharts 10.3.3ValuesChart context menuASIC1pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 Mouse02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuAngiotensin-converting enzyme 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCathepsin BpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuDiamine oxidasepKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • furin, paired basic amino acid cleaving enzyme/Furin in Human [ChEMBL: CHEMBL2611] [GtoPdb: 2366] [UniProtKB: P09958]
Created with Highcharts 10.3.3ValuesChart context menuFurinpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuPlasmodium falciparumpKd Plasmodium falciparumpKi Plasmodium falciparumpIC50 Plasmodium falciparumpEC50 Plasmodium falciparum02468Highcharts.com
  • Spermidine/spermine N(1)-acetyltransferase 1 in Human [ChEMBL: CHEMBL4286] [UniProtKB: P21673]
Created with Highcharts 10.3.3ValuesChart context menuSpermidine/spermine N(1)-acetyltransferase 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
Created with Highcharts 10.3.3ValuesChart context menuASIC2pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
  • ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
Created with Highcharts 10.3.3ValuesChart context menuASIC3pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
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]
Angiotensin-converting enzyme 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3736] [GtoPdb: 1614] [UniProtKB: Q9BYF1]
ChEMBL Activation of recombinant human ACE2 using McaAPK(Dnp)-OH as substrate preincubated for 15 mins followed by substrate addition spectra max Gemini M5 fluorescence plate reader analysis B 5.09 pEC50 8040 nM EC50 RSC Med Chem (2023) 14: 2206-2230 [PMID:37974956]
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]
furin, paired basic amino acid cleaving enzyme/Furin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2611] [GtoPdb: 2366] [UniProtKB: P09958]
ChEMBL Inhibition of furin (unknown origin) using Pyr-RTKR-MCA as substrate incubated for 30 mins and measured by FRET assay B 5.27 pKi 5420 nM Ki J Med Chem (2022) 65: 2747-2784 [PMID:34340303]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
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 35:

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]