mesoridazine [Ligand Id: 7227] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1088 (Mesoridazina, Mesoridazine, NC-123, NSC-186066, Serentil, Thioridazine-2-sulfoxide, TPS-23)
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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  • D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
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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 Inhibitory concentration against potassium channel HERG B 6.26 pIC50 549.54 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.49 pIC50 323.59 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 6.49 pIC50 323.59 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Inhibition of human ERG channel B 6.49 pIC50 320 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 6.49 pIC50 320 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG B 6.5 pIC50 316.23 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 6.98 pKi 105 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.26 pKi 55 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 6.39 pKi 412 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]
D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728]
GtoPdb - - 6.99 pKi 103 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]
D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 8.66 pKi 2.2 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]
D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 7.64 pKi 23 nM Ki Bioorg Med Chem Lett (2004) 14: 4379-82 [PMID:15357957]

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]