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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 |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]