vilazodone [Ligand Id: 7427] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL439849 (EMD 515259, EMD-515259, EMD-68-843, Vilazodone) |
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| 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-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 (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] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
