emetine [Ligand Id: 11087] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL50588 (6',7',10,11-tetramethoxyemetan, Cephaeline methyl ether, Emetan, 6',7',10,11-tetramethoxy-, Emetin, (-)-emetine, Emetine, Emetinum, GNF-Pf-196, NSC-33669, TCMDC-125531) |
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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 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]
