mizolastine [Ligand Id: 10102] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL94454 (Mizolastine, Mizollen)
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor in Guinea pig [GtoPdb: 262]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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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 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]