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

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ChEMBL ligand: CHEMBL1088 (Mesoridazine, Serentil, TPS-23, Lidanar, NC-123)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
1 CHEMBL1088_lig_chart_1 HERG Human
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • This target only has 1 pki data point
  • 6.98
2 CHEMBL1088_lig_chart_2 5-HT1A receptor Human
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 7.26
3 CHEMBL1088_lig_chart_3 5-HT2A receptor Human
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
  • 6.39
4 CHEMBL1088_lig_chart_4 5-HT2C receptor Human
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  • D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728]
  • This target only has 1 pki data point
  • 6.99
5 CHEMBL1088_lig_chart_5 D1 receptor Human
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  • D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416]
  • This target only has 1 pki data point
  • 8.66
6 CHEMBL1088_lig_chart_6 D2 receptor Human
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
  • This target only has 1 pki data point
  • 7.64
7 CHEMBL1088_lig_chart_7 D3 receptor Human
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]