emetine [Ligand Id: 11087] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL50588 (Emetine, TCMDC-125531, GNF-Pf-196)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
  • This target only has 1 pki data point
  • 5.58
1 CHEMBL50588_lig_chart_1 Alpha-1a adrenergic receptor Rat
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
  • This target only has 1 pki data point
  • 5.97
2 CHEMBL50588_lig_chart_2 Alpha-1b adrenergic receptor Rat
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • This target only has 1 pki data point
  • 7.85
3 CHEMBL50588_lig_chart_3 Alpha-2a adrenergic receptor Human
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
  • This target only has 1 pki data point
  • 7.59
4 CHEMBL50588_lig_chart_4 Alpha-2c adrenergic receptor Human
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  • Glucose transporter in Leishmania mexicana [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
  • Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
  • This target only has 0 pki data point
  • 0
5 CHEMBL50588_lig_chart_5 Glucose transporter Leishmania mexicanaHuman
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  • Hexose transporter 1 in Plasmodium falciparum [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
  • This target only has 0 pki data point
  • 0
6 CHEMBL50588_lig_chart_6 Hexose transporter 1 Plasmodium falciparum
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7 CHEMBL50588_lig_chart_7 NS5 Zika virus
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  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 0 pki data point
  • 0
8 CHEMBL50588_lig_chart_8 P-glycoprotein 1 Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
9 CHEMBL50588_lig_chart_9 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium yoelii [ChEMBL: CHEMBL612889]
  • This target only has 0 pki data point
  • 0
10 CHEMBL50588_lig_chart_10 Plasmodium yoelii Plasmodium yoelii
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  • RB binding protein 9, serine hydrolase/Putative hydrolase RBBP9 in Human [ChEMBL: CHEMBL1075121] [GtoPdb: 2874] [UniProtKB: O75884]
  • This target only has 0 pki data point
  • 0
11 CHEMBL50588_lig_chart_11 Putative hydrolase RBBP9 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.58 pKi 2642 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.19 pIC50 6527 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 5.97 pKi 1071 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.71 pIC50 1934 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 7.85 pKi 14 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) B 7.42 pIC50 38 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 7.59 pKi 26 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.74 pIC50 182 nM IC50 DrugMatrix in vitro pharmacology data
Glucose transporter in Leishmania mexicana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGT2 that are glucose transport deficient and complemented with the L. Mexicana glucose transporter 2. Activity is measured by by DNA content using SYBR green in vitro F 7.09 pIC50 81 nM IC50 St. Jude Leishmania screening dataset.
Glucose transporter 1/Glucose transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro F 6.97 pIC50 108 nM IC50 St. Jude Leishmania screening dataset.
Hexose transporter 1 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmPfHT that are glucose transport deficient and complemented with the Plasmodium falciparum hexose transporter. Activity is measured by by DNA content using SYBR green in vitro F 7.05 pIC50 90 nM IC50 St. Jude Leishmania screening dataset.
NS5 in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523952] [UniProtKB: A0A143MHK7]
ChEMBL Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in HEK293 cells assessed as antiviral activity by measuring NS1 protein expression preincubated for 1 hr followed by viral infection and measured after 24 hrs by TR-FRET assay B 7.28 pEC50 52.9 nM EC50 J Med Chem (2020) 63: 470-489 [PMID:31549836]
ChEMBL Inhibition of RNA-dependent RNA polymerase in Zika virus PRVABC59 infected in African green monkey Vero cells infected with supernatants from virus-infected human SNB-19 cells treated with compound for 1 hr assessed as antiviral activity after 48 to 72 hrs B 8.06 pEC50 8.74 nM EC50 J Med Chem (2020) 63: 470-489 [PMID:31549836]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells F 4.45 pIC50 35100 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 5.02 pIC50 9600 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.04 pIC50 9200 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.62 pIC50 2400 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay F 7.64 pEC50 22.94 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay F 7.99 pEC50 10.15 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
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 8.13 pIC50 7.49 nM IC50 Science (2011) 334: 1372-1377 [PMID:22096101]
RB binding protein 9, serine hydrolase/Putative hydrolase RBBP9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075121] [GtoPdb: 2874] [UniProtKB: O75884]
ChEMBL Displacement of fluorophosphate-rhodamine from RBBP9 transfected in human HEK293T cells proteomes after 30 mins by SDS-PAGE gel fluorescence assay B 5.11 pIC50 7800 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2254-2258 [PMID:20207142]

ChEMBL data shown on this page come from version 28:

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]