vilazodone [Ligand Id: 7427] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL439849 (EMD 515259, EMD-515259, EMD-68-843, Vilazodona, Vilazodone) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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/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] |
| DAT/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/Norepinephrine 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] |
| 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-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 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 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/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 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/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: 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] |
| 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 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/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 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 [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 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]
