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

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ChEMBL ligand: CHEMBL439849 (EMD 515259, EMD-515259, EMD-68-843, Emd-68843 base, EMD 68843 BASE, Vilazodona, Vilazodone)
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Rat [ChEMBL: CHEMBL5450] [GtoPdb: 3] [UniProtKB: P28565]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Rat [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Rat [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
  • D3 receptor/D(3) dopamine receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
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  • D4 receptor/D(4) dopamine receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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  • NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • SERT/Sodium-dependent serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
  • SERT/Sodium-dependent serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
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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
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]8-OH-DAPT from 5-HT1A receptor in human HEK293 cells measured after 60 mins by scintillation counting method B 7.55 pKi 28 nM Ki Bioorg Med Chem Lett (2022) 76: 129006-129006 [PMID:36202190]
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 F 9.7 pIC50 0.2 nM IC50 J Med Chem (2018) 61: 5822-5880 [PMID:29400967]
ChEMBL Inhibition of 5-HT1a (unknown origin) B 9.96 pIC50 0.11 nM IC50 Eur J Med Chem (2021) 223: 113644-113644 [PMID:34182358]
ChEMBL Agonist activity at 5-HT1AR (unknown origin) by Ultra Lance assay F 8.99 pEC50 1.02 nM EC50 Eur J Med Chem (2024) 275: 116564-116564 [PMID:38875810]
ChEMBL Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay F 9.1 pEC50 0.79 nM EC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
ChEMBL Agonist activity at recombinant human 5-HT1AR extracted from CHO cell membrane in presence of [35S]GTPgammaS by by liquid scintillation counting method F 9.52 pEC50 0.3 nM EC50 Eur J Med Chem (2024) 275: 116564-116564 [PMID:38875810]
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 F 9.92 pEC50 0.12 nM EC50 Bioorg Med Chem (2019) 27: 895-930 [PMID:30744931]
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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 8.36 pIC50 4.4 nM IC50 J Med Chem (2004) 47: 4684-4692 [PMID:15341484]
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/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Agonist activity at 5-HT1B receptor (unknown origin) F 4.52 pEC50 >30000 nM EC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
5-HT1B receptor/5-hydroxytryptamine receptor 1B 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/5-hydroxytryptamine receptor 1D 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2C 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-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/5-hydroxytryptamine receptor 4 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/5-hydroxytryptamine receptor 6 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/5-hydroxytryptamine receptor 7 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/5-hydroxytryptamine receptor 7 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]
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836]
ChEMBL Inhibition of AChE in mouse cortical homogenate using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method B 4.67 pIC50 21300 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
acetylcholinesterase (Yt 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/D(2) dopamine 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/D(2) dopamine 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]
ChEMBL Displacement of [3H]spiperone from dopamine D2 receptor of rat striatal membranes B 7.02 pIC50 95 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/D(3) dopamine 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/D(4) dopamine 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-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Inhibition against rat hydroxytryptamine 3 receptor B 5.37 pIC50 4300 nM IC50 J Med Chem (2004) 47: 4684-4692 [PMID:15341484]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of dopamine transporter (unknown origin) B 6.53 pIC50 295 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Inhibition of norepinephrine transporter (unknown origin) B 6.8 pIC50 158.1 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
SERT/Sodium-dependent 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]
ChEMBL Inhibition of human SERT expressed in HEK293 cells incubated for 30 mins B 9.17 pIC50 0.67 nM IC50 Eur J Med Chem (2024) 275: 116564-116564 [PMID:38875810]
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 receptor (unknown origin) B 9.32 pIC50 0.48 nM IC50 J Med Chem (2023) 66: 371-383 [PMID:36598095]
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]
ChEMBL Inhibition of SERT (unknown origin) in HEK293 cells assessed as inhibition of 5-HT reuptake by spectrophotometric analysis B 9.4 pIC50 0.4 nM IC50 Eur J Med Chem (2022) 229: 114045-114045 [PMID:34922191]
ChEMBL Inhibition of SERT (unknown origin) expressed in human HEK293 cells B 9.4 pIC50 0.4 nM IC50 Eur J Med Chem (2022) 236: 114347-114347 [PMID:35430560]
SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of serotonin transporter in rat brain tissue assessed as inhibition of [3H]-5-hydroxytryptamine reuptake B 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2022) 76: 129006-129006 [PMID:36202190]
ChEMBL Inhibition of [3H]5-HT re-uptake in rat synaptosomes B 8.96 pIC50 1.1 nM IC50 J Med Chem (2004) 47: 4684-4692 [PMID:15341484]
ChEMBL Inhibition of serotonin transporter expressed in rat brain tissue assessed as inhibition of [3H]-5-hydroxytryptamine reuptake measured after 15 mins by scintillation counting analysis B 9.17 pIC50 0.67 nM IC50 Eur J Med Chem (2021) 223: 113644-113644 [PMID:34182358]
ChEMBL Inhibition of SERT in rat cerebral synaptosomes assessed as reduction in [3H]5-HT uptake B 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2024) 275: 116564-116564 [PMID:38875810]
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]
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]
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 36:

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]