diminazene [Ligand Id: 10307] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL35241 (4,4'-(diazoamino)benzamidine, Diminazen, Diminazene, Diminazeno) |
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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] |
| 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 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]
