epinastine [Ligand Id: 7176] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1106 (Elestat, Epinastine, Purivist, WAL-801) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 4 | pIC50 | 100000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 4 | pIC50 | 100000 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 4.04 | pIC50 | 91201.08 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389] | ||||||||
| ChEMBL | Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig cerebellum membranes after 30 min | B | 8.85 | pKi | 1.41 | nM | Ki | J Med Chem (1995) 38: 3351-3360 [PMID:7650688] |
| ChEMBL | Potency against histamine H1 receptor on guinea pig ileum | B | 8.8 | pIC50 | 1.58 | nM | IC50 | J Med Chem (1995) 38: 3351-3360 [PMID:7650688] |
| 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 | 5.96 | pIC50 | 1100 | 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 | 4.53 | pIC50 | 29800 | 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 | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| GtoPdb | Antagonism of 5 nM [3H]mepyramine binding in an intact cell assay using U373 MG astrocytoma cells. | - | 7.6 | pIC50 | 25 | nM | IC50 | J Pharmacol Sci (2008) 107: 66-79 [PMID:18446005] |
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]
