vortioxetine [Ligand Id: 7351] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2104993 (LU AA21004, Brintellix, Vortioxetine, LUAA21004, LU-AA21004)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
1 CHEMBL2104993_lig_chart_1 Serotonin 1a (5-HT1a) receptor Human
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
2 CHEMBL2104993_lig_chart_2 Serotonin 7 (5-HT7) receptor Human
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  • SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
  • SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
  • This target only has 1 pki data point
3 CHEMBL2104993_lig_chart_3 SERT HumanRat
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
  • This target only has 1 pki data point
4 CHEMBL2104993_lig_chart_4 5-HT1B receptor Human
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  • 5-HT1D receptor in Rat [GtoPdb: 3] [UniProtKB: P28565]
  • This target only has 0 pki data point
5 CHEMBL2104993_lig_chart_5 5-HT1D receptor Rat
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
6 CHEMBL2104993_lig_chart_6 5-HT2A receptor Human
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  • 5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
  • This target only has 1 pki data point
7 CHEMBL2104993_lig_chart_7 5-HT5A receptor Human
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • This target only has 1 pki data point
8 CHEMBL2104993_lig_chart_8 5-HT6 receptor Human
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  • 5-HT3A in Human [GtoPdb: 379]
  • This target only has 1 pki data point
9 CHEMBL2104993_lig_chart_9 5-HT3A Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.82 pKi 15 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method B 8.02 pKi 9.5 nM Ki Bioorg Med Chem Lett (2017) 27: 5420-5423 [PMID:29138029]
ChEMBL Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 mins by TopCount scintillation counting method B 8.02 pKi 9.5 nM Ki Eur J Med Chem (2018) 144: 701-715 [PMID:29291438]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
GtoPdb - - 6.35 pKi 450 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
ChEMBL Displacement of [3H]-LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes measured after 60 mins by scintillation counting method B 7.59 pKi 26 nM Ki Bioorg Med Chem Lett (2017) 27: 5420-5423 [PMID:29138029]
ChEMBL Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method B 7.59 pKi 26 nM Ki Eur J Med Chem (2018) 144: 701-715 [PMID:29291438]
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb - - 8.8 pKi 1.6 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of SERT in rat brain synaptosomes assessed as reduction in [3H]-5-HT uptake measured after 15 mins by scintillation counting method B 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem Lett (2017) 27: 5420-5423 [PMID:29138029]
ChEMBL Inhibition of [3H]serotonin reuptake in rat brain synaptosomes SERT after 15 mins by TopCount scintillation counting method B 8.54 pIC50 2.9 nM IC50 Eur J Med Chem (2018) 144: 701-715 [PMID:29291438]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 7.48 pKi 33 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
5-HT1D receptor in Rat [GtoPdb: 3] [UniProtKB: P28565]
GtoPdb - - 5.4 pIC50 4000 nM IC50 J. Med. Chem. (2004) 47: 4684-92 [PMID:15341484]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 6.74 pKi 180 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
5-HT5A receptor in Human [GtoPdb: 10] [UniProtKB: P47898]
GtoPdb - - 6.66 pKi 220 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 6.48 pKi 330 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]
5-HT3A in Human [GtoPdb: 379]
GtoPdb - - 8.43 pKi 3.7 nM Ki J. Med. Chem. (2011) 54: 3206-21 [PMID:21486038]

ChEMBL data shown on this page come from version 27:

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]