vilazodone [Ligand Id: 7427] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL439849 (EMD 515259, EMD-515259, Vilazodone, EMD-68-843)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Rat [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
ChEMBL Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method B 4.67 pIC50 21300 nM IC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
ChEMBL Inhibition of rat cortex acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 4.67 pIC50 21300 nM IC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting B 6.18 pKi 666 nM Ki Eur. J. Med. Chem. (2012) 53: 124-132 [PMID:22520153]
GtoPdb - - 6.18 pIC50 666 nM IC50 J Med Chem (2004) 47: 4684-92 [PMID:15341484]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor of rat striatal membranes B 6.18 pIC50 666 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 7.15 pIC50 71 nM IC50 J Med Chem (2004) 47: 4684-92 [PMID:15341484]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Inhibition of rat dopamine D3 receptor B 7.15 pIC50 71 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
ChEMBL Inhibition of rat dopamine D4 receptor B 5.47 pIC50 3400 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in CHO-K1 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 8.01 pKi 9.7 nM Ki Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL Displacement of [3H]8-OH-DPAT from human 5HT1A receptor by liquid scintillation counting B 9.52 pKi 0.3 nM Ki Eur. J. Med. Chem. (2012) 53: 124-132 [PMID:22520153]
ChEMBL Displacement of [3H]-8-OH-DPAT from 5HT1A receptor (unknown origin) expressed in HEK293 cells membranes incubated for 60 mins by scintillation counting method B 9.7 pKi 0.2 nM Ki Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993]
GtoPdb Binding of vilazodone to human 5-HT1A receptors against [3H]8-OH-DPAT (DPAT) - 9.7 pKi 0.2 nM Ki CNS Neurosci Ther (2009) 15: 107-17 [PMID:19499624]
GtoPdb - - 9.52 pIC50 0.3 nM IC50 J Med Chem (2004) 47: 4684-92 [PMID:15341484]
ChEMBL Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method B 9.7 pIC50 0.2 nM IC50 J Med Chem (2018) 61: 5822-5880 [PMID:29400967]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay F 9.92 pEC50 0.12 nM EC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
ChEMBL Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay B 9.92 pEC50 0.12 nM EC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Inhibition of 8-OH DPAT binding to rat hydroxytryptamine 1A receptor expressed in CHO cells B 9.52 pIC50 0.3 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL Inhibition of rat hydroxytryptamine 1B receptor B 5.3 pIC50 5000 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
ChEMBL Inhibition of rat hydroxytryptamine 1D receptor B 5.4 pIC50 4000 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Inhibition of rat hydroxytryptamine 2A receptor B 5.82 pIC50 1510 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Inhibition of rat hydroxytryptamine 2C receptor B 5.7 pIC50 2000 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Inhibition against rat hydroxytryptamine 3 receptor B 5.37 pIC50 4300 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
GtoPdb - - 6.6 pIC50 252 nM IC50 J Med Chem (2004) 47: 4684-92 [PMID:15341484]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL Inhibition of rat hydroxytryptamine 4 receptor B 6.6 pIC50 252 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
ChEMBL Inhibition of rat hydroxytryptamine 6 receptor B 5.52 pIC50 3000 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method B 5.41 pKi 3900 nM Ki Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Inhibition of rat hydroxytryptamine 7 receptor B 5.52 pIC50 3000 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK293 cells membranes incubated for 30 mins by microbeta scintillation counting analysis B 8.72 pKi 1.9 nM Ki Eur J Med Chem (2019) 183: 111736-111736 [PMID:31586817]
ChEMBL Displacement of [3H]Citalopram from human SERT by liquid scintillation counting B 9.3 pKi 0.5 nM Ki Eur. J. Med. Chem. (2012) 53: 124-132 [PMID:22520153]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 CNS Neurosci Ther (2009) 15: 107-17 [PMID:19499624];
J Med Chem (2004) 47: 4684-92 [PMID:15341484]
ChEMBL Inhibition of SERT (unknown origin) expressed in HEK293 cells assessed as reduction in 5-HT uptake incubated for 30 mins B 9.4 pIC50 0.4 nM IC50 Bioorg Med Chem (2018) 26: 3117-3125 [PMID:29729987]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of [3H]5-HT re-uptake in rat synaptosomes B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2004) 47: 4684-4692 [PMID:15341484]
ChEMBL inhibition of rat cerebral 5HT transporter assessed as reduction in [3H]5HT reuptake after 4 mins B 9.3 pIC50 0.5 nM IC50 J Med Chem (2018) 61: 5822-5880 [PMID:29400967]
ChEMBL Inhibition of rat synaptosomes 5HT transporter assessed as reduction in [3H]serotonin reuptake incubated for 15 mins by scintillation counting method B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 6.5 pIC50 317 nM IC50 J Med Chem (2004) 47: 4684-92 [PMID:15341484]

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]