ChEMBL ligand: CHEMBL53463 (Adriablastin, Adriamycin, Adriblastina, Doxil, Doxorubicin, Epirubicin hydrochloride impurity, doxorubicin-, Hydroxydaunorubicin, NSC-123127, NSC-759155, Rubex, Valrubicin impurity, doxorubicin)
Anti-estrogen binding site (AEBS) in Human [ChEMBL: CHEMBL612409] [UniProtKB: Q15125, Q9UBM7] There should be some charts here, you may need to enable JavaScript!
Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530] There should be some charts here, you may need to enable JavaScript!
Carnitine palmitoyltransferase 2 in Rat [ChEMBL: CHEMBL4037] [UniProtKB: P18886] There should be some charts here, you may need to enable JavaScript!
Caspase 1/Caspase-1 in Human [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466] There should be some charts here, you may need to enable JavaScript!
CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] There should be some charts here, you may need to enable JavaScript!
DNA (cytosine-5-)-methyltransferase 3α/DNA (cytosine-5)-methyltransferase 3A in Mouse [ChEMBL: CHEMBL3108652] [GtoPdb: 2750] [UniProtKB: O88508] There should be some charts here, you may need to enable JavaScript!
DNA topoisomerase I in Human [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387] There should be some charts here, you may need to enable JavaScript!
DNA topoisomerase II alpha in Human [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388] There should be some charts here, you may need to enable JavaScript!
DNA topoisomerase II beta in Human [ChEMBL: CHEMBL3396] [UniProtKB: Q02880] There should be some charts here, you may need to enable JavaScript!
Human immunodeficiency virus type 1 integrase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL3471] [UniProtKB: Q7ZJM1] There should be some charts here, you may need to enable JavaScript!
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 [ChEMBL: CHEMBL247] [UniProtKB: Q72547] There should be some charts here, you may need to enable JavaScript!
MMP2/Matrix metalloproteinase-2 in Human [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253] There should be some charts here, you may need to enable JavaScript!
ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] There should be some charts here, you may need to enable JavaScript!
Plasmodium berghei [ChEMBL: CHEMBL612653] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244] There should be some charts here, you may need to enable JavaScript!
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626] There should be some charts here, you may need to enable JavaScript!
Ribonuclease pancreatic in Bovine [ChEMBL: CHEMBL6091] [UniProtKB: P61823] There should be some charts here, you may need to enable JavaScript!
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] There should be some charts here, you may need to enable JavaScript!
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] There should be some charts here, you may need to enable JavaScript!
Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528] There should be some charts here, you may need to enable JavaScript!
Telomerase reverse transcriptase in Human [ChEMBL: CHEMBL2916] [UniProtKB: O14746] There should be some charts here, you may need to enable JavaScript!
Type-2 restriction enzyme HindIII in Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) [ChEMBL: CHEMBL5004] [UniProtKB: P43870] There should be some charts here, you may need to enable JavaScript!
Type-2 restriction enzyme ScaI in Streptomyces caespitosus [ChEMBL: CHEMBL5782] [UniProtKB: O52691] There should be some charts here, you may need to enable JavaScript!
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] There should be some charts here, you may need to enable JavaScript!
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] 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
Anti-estrogen binding site (AEBS) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL612409] [UniProtKB: Q15125, Q9UBM7]
ChEMBL	Growth inhibition of MDA-MB-231 cells containing antiestrogen binding sites	F	6.52	pIC50	300	nM	IC50	J. Med. Chem. (2004) 47: 6509-6518 [PMID:15588086]
ChEMBL	Growth inhibition of MCF7 cells expressing ER and antiestrogen binding sites	F	6.7	pIC50	200	nM	IC50	J. Med. Chem. (2004) 47: 6509-6518 [PMID:15588086]
ChEMBL	Growth inhibition of MDA-MB-435 cells containing antiestrogen binding sites	F	6.82	pIC50	150	nM	IC50	J. Med. Chem. (2004) 47: 6509-6518 [PMID:15588086]
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL	DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)	B	4.87	pIC50	13590	nM	IC50	DrugMatrix in vitro pharmacology data
Carnitine palmitoyltransferase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4037] [UniProtKB: P18886]
ChEMBL	Inhibition of rat CPT2 in rat mitochondria	B	4	pIC50	>100000	nM	IC50	J. Med. Chem. (2011) 54: 3109-3152 [PMID:21504156]
Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466]
ChEMBL	DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)	B	4.91	pIC50	12192	nM	IC50	DrugMatrix in vitro pharmacology data
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
ChEMBL	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis	B	5.46	pKi	3451	nM	Ki	Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
ChEMBL	Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay	B	4.09	pIC50	80760	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
DNA (cytosine-5-)-methyltransferase 3α/DNA (cytosine-5)-methyltransferase 3A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108652] [GtoPdb: 2750] [UniProtKB: O88508]
ChEMBL	Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition	B	5.52	pIC50	3000	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127296-127296 [PMID:32631516]
DNA topoisomerase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781] [GtoPdb: 2636] [UniProtKB: P11387]
ChEMBL	Inhibition of human topoisomerase 1 assessed as decrease in pBR322 mobility on agarose gel by electrophoresis	B	4.7	pIC50	20000	nM	IC50	J. Med. Chem. (2010) 53: 6164-6179 [PMID:20662543]
DNA topoisomerase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1806] [GtoPdb: 2637] [UniProtKB: P11388]
ChEMBL	Inhibition of human DNA topoisomerase 2alpha-mediated decatenation of kinetoplast DNA after 60 mins by agarose gel electrophoresis	B	5.52	pIC50	3000	nM	IC50	Eur J Med Chem (2016) 123: 704-717 [PMID:27521587]
ChEMBL	Inhibition of human topoisomerase 2alpha-mediated kinetoplast DNA decatenation after 60 mins by ethidium bromide staining based agarose gel electrophoresis	B	5.52	pIC50	3000	nM	IC50	Bioorg Med Chem (2017) 25: 2625-2634 [PMID:28342691]
GtoPdb	In vitro inhibition of DNA relaxation and decatenation activities in a topoisomerase extract from human placenta.	-	6	pIC50	1000	nM	IC50	J Nat Prod (2001) 64: 204-7 [PMID:11430001]
ChEMBL	Inhibition human placenta topoisomerase 2 assessed as conversion of supercoiled pBR322 DNA to relaxed form	B	6	pIC50	1000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
ChEMBL	Inhibition human placenta topoisomerase 2 assessed as conversion of catenated kinetoplast DNA to minicircle monomer	B	6	pIC50	1000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
ChEMBL	Inhibition of human topoisomerase-2 alpha in human A498 cells assessed as decrease in relaxation of supercoiled DNA at 10 uM	B	6	pIC50	990	nM	IC50	Bioorg Med Chem Lett (2021) 40: 127916-127916 [PMID:33689875]
ChEMBL	Inhibition of human topoisomerase 2 using supercoiled pHOT1 DNA as substrate after 30 mins by agarose gel electrophoresis	B	6.06	pIC50	880	nM	IC50	Eur J Med Chem (2018) 155: 117-134 [PMID:29885574]
DNA topoisomerase II beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3396] [UniProtKB: Q02880]
ChEMBL	Inhibition of human topoisomerase-2B after 2 hrs by ELISA	B	5.46	pIC50	3500	nM	IC50	Eur J Med Chem (2018) 150: 403-418 [PMID:29547830]
ChEMBL	Inhibition of human topoisomerase 2beta after 2 hrs at 37 degC by ELISA	B	5.46	pIC50	3500	nM	IC50	Eur J Med Chem (2018) 143: 1807-1825 [PMID:29133058]
ChEMBL	Inhibition of Topoisomerase II beta (unknown origin) relative to control	B	6.14	pIC50	727	nM	IC50	Bioorg Med Chem (2020) 28: 115674-115674 [PMID:33065442]
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	5.62	pIC50	2400	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	6.05	pIC50	900	nM	IC50	J. Med. Chem. (2000) 43: 2100-2114 [PMID:10841789]
Human immunodeficiency virus type 1 reverse transcriptase in Human immunodeficiency virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL247] [UniProtKB: Q72547]
ChEMBL	Inhibition of HIV-1 reverse transcriptase using Poly(rA).p(dT) (12 to 18) as substrate after 30 mins by single point PCR assay	B	4.28	pIC50	52000	nM	IC50	Bioorg. Med. Chem. Lett. (2012) 22: 4844-4848 [PMID:22695131]
MMP2/Matrix metalloproteinase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL333] [GtoPdb: 1629] [UniProtKB: P08253]
ChEMBL	Inhibitory concentration against Clostridium histolyticum Collagenase	B	5.96	pIC50	1100	nM	IC50	J. Med. Chem. (1992) 35: 2768-2771 [PMID:1322986]
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL	TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.05 uM) in membrane vesicle from MRP1-expressing HeLa cells	F	4.3	pIC50	50000	nM	IC50	J. Biol. Chem. (1996) 271: 9683-9689 [PMID:8621644]
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	5.43	pKi	3693	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	4.81	pIC50	15336	nM	IC50	DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL	TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells	F	5.07	pKi	8500	nM	Ki	Pharm. Res. (2001) 18: 171-176 [PMID:11405287]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	F	6.05	pIC50	886	nM	IC50	Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	HARVARD: Inhibition of blood stage Plasmodium falciparum Dd2 infection	F	7.24	pIC50	58	nM	IC50	Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
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	5.6	pIC50	2485	nM	IC50	DrugMatrix in vitro pharmacology data
Ribonuclease pancreatic in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6091] [UniProtKB: P61823]
ChEMBL	Inhibition of bovine pancreas RNase A assessed as undigested supercoiled pBR322 DNA concentration	B	4.6	pIC50	25000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL	Inhibition of GST-tagged Aurora A kinase expressed in insect cells assessed as inhibition of [33P]gamma-ATP incorporation in substrate after 60 mins by scintillation counting	B	7.4	pIC50	40	nM	IC50	Eur. J. Med. Chem. (2011) 46: 3690-3695 [PMID:21664013]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	4.81	pKi	15666	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	4.46	pIC50	34464	nM	IC50	DrugMatrix in vitro pharmacology data
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)	B	5.68	pKi	2078	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)	B	4.9	pIC50	12468	nM	IC50	DrugMatrix in vitro pharmacology data
Telomerase reverse transcriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2916] [UniProtKB: O14746]
ChEMBL	Inhibition of telomerase from human COLO201 cell	B	4.14	pIC50	73000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
Type-2 restriction enzyme HindIII in Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5004] [UniProtKB: P43870]
ChEMBL	Inhibition of Haemophilus influenzae Hind 3 assessed as undigested supercoiled pBR322 DNA concentration	B	4.02	pIC50	96000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
Type-2 restriction enzyme ScaI in Streptomyces caespitosus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5782] [UniProtKB: O52691]
ChEMBL	Inhibition of Streptomyces caespitosus Sca 1 assessed as undigested supercoiled pBR322 DNA concentration	B	4.6	pIC50	25000	nM	IC50	J. Nat. Prod. (2001) 64: 204-207 [PMID:11430001]
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	5.29	pIC50	5147	nM	IC50	DrugMatrix in vitro pharmacology data
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL	DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))	B	4.5	pIC50	31913	nM	IC50	DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]