mepacrine [Ligand Id: 10172] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL7568 (Mepacrine, Quinacrine, GNF-Pf-5448)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • Trypanothione reductase in Trypanosoma cruzi [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) B 5.57 pIC50 2667 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.72 pKi 1890 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.47 pIC50 3414 nM IC50 DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.99 pKi 1015 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) B 5.69 pIC50 2065 nM IC50 DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 6.07 pKi 855 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 5.64 pIC50 2280 nM IC50 DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 6.08 pKi 833 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) B 5.74 pIC50 1825 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.25 pKi 560 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.41 pIC50 3857 nM IC50 DrugMatrix in vitro pharmacology data
Bacterial DNA-directed RNA polymerase in Bacteria (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2364672] [UniProtKB: P0A7Z4P0A800P0A8T7P0A8V2]
ChEMBL Inhibition of Escherichia coli DNA-primed RNA polymerase activity using [8-14C]ATP by scintillation counting B 4.7 pIC50 20000 nM IC50 J. Med. Chem. (1976) 19: 994-998 [PMID:184284]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay B 5.35 pIC50 4500 nM IC50 Eur. J. Med. Chem. (2011) 46: 2170-2184 [PMID:21459491]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.35 pKi 448 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.88 pIC50 1318 nM IC50 DrugMatrix in vitro pharmacology data
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.46 pKi 3476 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) B 5.45 pIC50 3535 nM IC50 DrugMatrix in vitro pharmacology data
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 6.44 pKi 359 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.83 pIC50 1489 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 6.46 pKi 343 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.02 pIC50 964 nM IC50 DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 6.58 pKi 266 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.9 pIC50 1255 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 6.56 pKi 277 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.7 pIC50 1983 nM IC50 DrugMatrix in vitro pharmacology data
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.57 pKi 2684 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) B 5.43 pIC50 3736 nM IC50 DrugMatrix in vitro pharmacology data
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 5.54 pKi 2872 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.54 pIC50 2896 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: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells F 4.84 pEC50 14400 nM EC50 Anticancer Drugs (1996) 7: 568-578 [PMID:8862725]
Phospholipase A2 group 1B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4715] [UniProtKB: P00592]
ChEMBL Tested for its inhibitory activity against Phospholipase A2 (PLA2) B 4 pIC50 100000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 2087-2092
sPLA2-1B/Phospholipase A2 group 1B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5016] [GtoPdb: 1416] [UniProtKB: P04055]
ChEMBL Inhibitory activity against polymorphonuclear cell phospholipase-A2 in rat B 4 pIC50 100000 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 711-716
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 4.39 pIC50 41000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimicrobial activity against chloroquine-resistant Plasmodium falciparum W2 after 72 hrs F 7.48 pEC50 33 nM EC50 Antimicrob. Agents Chemother. (2007) 51: 2164-2172 [PMID:17371810]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay F 7.85 pEC50 14.22 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs F 7.96 pEC50 11 nM EC50 Antimicrob. Agents Chemother. (2007) 51: 2164-2172 [PMID:17371810]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay F 8.09 pEC50 8.13 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method F 7.89 pIC50 13 nM IC50 Med Chem Res (2007) 16: 213-229
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs by [G-3H]hypoxanthine uptake F 7.37 pIC50 43 nM IC50 Eur. J. Med. Chem. (2008) 43: 2840-2852 [PMID:18395298]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as incorporation of [3H]hypoxanthine after 48 hr microdilution method F 7.37 pIC50 43 nM IC50 Med Chem Res (2007) 16: 213-229
ChEMBL Effective concentration against Plasmodium falciparum W2 F 7.49 pEC50 32 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 1015-1018 [PMID:15686903]
ChEMBL Effective concentration against Plasmodium falciparum W2 F 8.1 pEC50 8 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 1015-1018 [PMID:15686903]
ChEMBL Effective concentration for Plasmodium falciparum 3D7 F 8.1 pEC50 8 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 1015-1018 [PMID:15686903]
ChEMBL Effective concentration for Plasmodium falciparum 3D7 F 8.3 pEC50 5 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 1015-1018 [PMID:15686903]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration F 6.78 pIC50 165.7 nM IC50 Science (2011) 334: 1372-1377 [PMID:22096101]
Plasmodium yoelii yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612328]
ChEMBL Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs F 4.52 pIC50 30000 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 1215-1220 [PMID:18212104]
Prion protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4869] [UniProtKB: P04156]
ChEMBL Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells B 6.52 pEC50 300 nM EC50 J. Med. Chem. (2003) 46: 3563-3564 [PMID:12904059]
Riboflavin-binding protein in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944489] [UniProtKB: P02752]
ChEMBL Binding affinity to chicken riboflavin binding protein assessed as dissociation constant at pH 7.4 in phosphate buffer by isothermal titration calorimetric assay B 6.58 pKd 264 nM Kd ACS Med. Chem. Lett. (2011) 2: 363-367 [PMID:21686082]
ChEMBL Competitive inhibition of chicken riboflavin binding protein by surface plasmon resonance assay B 5.17 pKi 6700 nM Ki ACS Med. Chem. Lett. (2011) 2: 363-367 [PMID:21686082]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.12 pKi 761 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 5.57 pIC50 2663 nM IC50 DrugMatrix in vitro pharmacology data
Trypanothione reductase in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5131] [UniProtKB: P28593]
ChEMBL The competitive inhibitory activity against trypanothione reductase was evaluated from Lineweaver Burk plots B 4.72 pKi 19000 nM Ki J. Med. Chem. (1999) 42: 5448-5454 [PMID:10639286]
ChEMBL Inhibition of Trypanosoma cruzi trypanothione reductase B 4.72 pKi 19000 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3031-3035 [PMID:19414258]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in guinea pig ventricular myocytes F 5.25 pIC50 5600 nM IC50 IC50 data for the L-type calcium channel extracted from a set of literature articles
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 5.28 pIC50 5200 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]