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

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ChEMBL ligand: CHEMBL94454 (Mizolastina, 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 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]