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ChEMBL ligand: CHEMBL94454 (Mizolastine, Mizollen) |
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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 | Displacement of [3H]dofetolide from human ERG channel expressed in HEK293 cells at 37 degC by liquid scintillation assay | B | 5.14 | pKi | 7258 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4380-4384 [PMID:19553115] |
ChEMBL | Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay | B | 6.36 | pIC50 | 441 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4380-4384 [PMID:19553115] |
ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 6.36 | pIC50 | 436.52 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
ChEMBL | Inhibitory concentration against potassium channel HERG | B | 6.36 | pIC50 | 436.52 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
ChEMBL | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 6.36 | pIC50 | 436.52 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
ChEMBL | Inhibition of human ERG | B | 6.36 | pIC50 | 436.52 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
ChEMBL | Inhibition of human ERG in MCF7 cells | B | 6.45 | pIC50 | 354.81 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
ChEMBL | Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) | F | 6.45 | pIC50 | 354.81 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831] |
ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation assay | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4380-4384 [PMID:19553115] |
GtoPdb | Radioligand displacement membrane binding assay using CHO cells expressing the human H1 receptor and [3H]pyrilamine as tracer. | - | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4380-4 [PMID:19553115] |
H1 receptor in Guinea pig [GtoPdb: 262] | ||||||||
GtoPdb | Inhibition of [3H]pyrilamine binding to histamine H1 receptors in guinea pig cerebellar membranes and sections. | - | 7.33 | pIC50 | 47 | nM | IC50 | Arzneimittelforschung (1995) 45: 551-8 [PMID:7612054] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Displacement of [3H]N-methyl Scopolamine from human muscarinic M1 receptor expressed in CHO Flp-In cells by liquid scintillation assay | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4380-4384 [PMID:19553115] |
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]