mitoxantrone [Ligand Id: 7242] 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: CHEMBL58 (Misostol, Mitoxantrona, Mitoxantrone, Mitoxantrone HCl, Novantrone, NSC-279836) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
| ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.75 | pIC50 | 1785.3 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of BCRP in human HEK293/R2 cells assessed as reduction in cell viability after 5 days by MTS/PMS assay | B | 6.04 | pIC50 | 903.8 | nM | IC50 | J Med Chem (2019) 62: 8578-8608 [PMID:31465686] |
| DNA topoisomerase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] | ||||||||
| ChEMBL | Inhibition of human topoisomerase 2alpha decantation activity | B | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem (2008) 16: 3959-3968 [PMID:18258442] |
| GtoPdb | Inhibition of topoisomerase IIα-mediated decatenation activity. | - | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem (2008) 16: 3959-68 [PMID:18258442] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 5.27 | pIC50 | 5385.9 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.53 | pKi | 2937 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole) | B | 5.45 | pIC50 | 3584.9 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1] | ||||||||
| ChEMBL | Tested for inhibition of HIV-1 integrase, under 1 uM for the strand transfer | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2000) 43: 2100-2114 [PMID:10841789] |
| ChEMBL | Inhibition of HIV-1 integrase, under 1 uM for the 3''-preprocessing | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2000) 43: 2100-2114 [PMID:10841789] |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 6.08 | pIC50 | 830 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] | ||||||||
| ChEMBL | Inhibition of MRP1 in human 2008/MRP1 cells assessed as reduction in cell viability after 5 days by MTS/PMS assay | B | 7.56 | pIC50 | 27.5 | nM | IC50 | J Med Chem (2019) 62: 8578-8608 [PMID:31465686] |
| ChEMBL | TP_TRANSPORTER: cell accumulation in MCF7/MRP1-10 cells | F | 8.72 | pIC50 | 1.9 | nM | IC50 | Mol Pharmacol (2006) 69: 1499-1505 [PMID:16434618] |
| ChEMBL | TP_TRANSPORTER: cell accumulation in MCF7/MRP1-M24 cells | F | 8.82 | pIC50 | 1.5 | nM | IC50 | Mol Pharmacol (2006) 69: 1499-1505 [PMID:16434618] |
| ChEMBL | TP_TRANSPORTER: cell accumulation in MCF7/MRP1-M6 cells | F | 8.82 | pIC50 | 1.5 | nM | IC50 | Mol Pharmacol (2006) 69: 1499-1505 [PMID:16434618] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.74 | pKi | 180.3 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.13 | pIC50 | 748.7 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.11 | pKi | 77.9 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.66 | pIC50 | 219 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.05 | pKi | 89.8 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 6.19 | pIC50 | 644.1 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NEDD8 activating enzyme in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3831283] [UniProtKB: Q13564, Q8TBC4] | ||||||||
| ChEMBL | Inhibition of NAE-mediated Ubcl2-NEDD8 conjugation in human Caco2 cells after 16 hrs by Western blot analysis | B | 5.89 | pEC50 | 1300 | nM | EC50 | Eur J Med Chem (2018) 143: 1021-1027 [PMID:29232579] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.31 | pKi | 4948.5 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.3 | pIC50 | 4989.8 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
| ChEMBL | Inhibition of MDR in human LCC6MDR cells assessed as reduction in cell viability after 5 days by MTS/PMS assay | B | 5.82 | pIC50 | 1501 | nM | IC50 | J Med Chem (2019) 62: 8578-8608 [PMID:31465686] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.8 | pIC50 | 1584.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.9 | pIC50 | 1258.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 6 | pIC50 | 1000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 6 | pIC50 | 1000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 6 | pIC50 | 1000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 6.1 | pIC50 | 794.33 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 6.2 | pIC50 | 630.96 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 8.83 | pIC50 | 1.48 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 8.85 | pIC50 | 1.41 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 8.95 | pIC50 | 1.12 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 9 | pIC50 | 1 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 9.03 | pIC50 | 0.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 9.08 | pIC50 | 0.83 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 9.23 | pIC50 | 0.59 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922] | ||||||||
| ChEMBL | Inhibition of ROS1 (unknown origin) using poly (Glu,Tyr)4:1 substrate and ATP incubated for 60 mins by ELISA | B | 5.52 | pIC50 | 2998.7 | nM | IC50 | Medchemcomm (2017) 8: 621-624 [PMID:30108778] |
| P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] | ||||||||
| ChEMBL | Displacement of [3H]PSB0413 from human platelet P2Y12 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 3784-3793 [PMID:19463000] |
| erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 5.69 | pIC50 | 2035.2 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.73 | pKi | 1865.7 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.45 | pIC50 | 3561.9 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.36 | pIC50 | 43900 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.13 | pIC50 | 73300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.22 | pIC50 | 60500 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| TAR DNA-binding protein 43 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2362981] [UniProtKB: Q13148] | ||||||||
| ChEMBL | Inhibition of TDP-43 (unknown origin) binding to RNA | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126942-126942 [PMID:31926785] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Inhibition of BTK (unknown origin) | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2013) 56: 2619-2629 [PMID:23442188] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 5.9 | pIC50 | 1257.9 | nM | IC50 | DrugMatrix in vitro pharmacology data |
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]
