mitoxantrone [Ligand Id: 7242] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL58 (Misostol, Mitoxantrone, Mitoxantrone HCl, Novantrone, NSC-279836) |
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| 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 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]
