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ChEMBL ligand: CHEMBL2104993 (Brintellix, LUAA21004, LU AA21004, LU-AA21004, Vortioxetine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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] |
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 | 8.02 | pKi | 9.5 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993] |
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 | 8.02 | pKi | 9.5 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126769-126769 [PMID:31699607] |
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] |
ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993] |
ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126769-126769 [PMID:31699607] |
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] |
ChEMBL | Inhibition of rat synaptosomes 5HT transporter assessed as reduction in [3H]serotonin reuptake incubated for 15 mins by scintillation counting method | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126703-126703 [PMID:31627993] |
ChEMBL | Inhibition of rat synaptosomes 5HT transporter assessed as reduction in [3H]serotonin reuptake incubated for 15 mins by scintillation counting method | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126769-126769 [PMID:31699607] |
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 32:
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]