ChEMBL ligand: CHEMBL1118 (Desvenlafaxina, Desvenlafaxine, D-veniz, Khedezla, Mdd-xr, Newven, O-desmethylvenlafaxine, O-desmethylvenlafaxine (odv), Odv)
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] There should be some charts here, you may need to enable JavaScript!
Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] There should be some charts here, you may need to enable JavaScript!
NET/Sodium-dependent noradrenaline transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
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] 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
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL	Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain	B	7.22	pIC50	60	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes	F	5.94	pIC50	1160	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	Uptake Assay Protocol: DAT: This protocol was designed to measure inhibition of uptake by the human dopamine transporter. The reagents were human DAT (HEK293F) cells, GBR 12909 (Sigma), nomifensine, neurotransmitter transporter uptake assay kit (Molecular Devices), freestyle 293 expression medium (Invitrogen), 10× Hank's Balanced Salt Solution (HBSS; Invitrogen), 1 M HEPES (Mediatech), Biocoat poly-D-lysine 96-well, black, clear plates (Becton, Dickinson), and 500 pt polypropylene U-bottom 96-well plates (Fisher). The Assay Buffer (AB) was 1×HBSS and 0.02 M HEPES.The HEK293F cells were transfected with the human dopamine transporter and frozen in 1 mL aliquots at about 1E+07 cells/mL. On the day of the experiment, the cells were removed from −80° C. or liquid nitrogen and thawed in a room temperature water bath. The cells were dilute to about 1-2E+06 with Freestyle medium. A 1 mL sample (1:2 dilution) was prepared, and the cells were counted. The cells were spun at 1100 rpm for 5 minutes, and the medium was aspirated off. The cells were resuspend in medium at 1.5E+06 cells/mL for about 60,000 cells per well. 40 μL of cells were dispensed per well in the Biocoat plates. The plates were spun at 1100 rpm for 1 minute to improve homogeneity of the cell layer and were incubated at 37° C. for a minimum of 3 hours.12 μL of test compound (10 mM) in DMSO was added to the wells, and nomifensine was used as a control. GBR 12909 (final assay concentration of 10 μM) was used for background signal. The neurotransmitter transporter dye was prepared in AB prior to use.	B	5.43	pKi	3726	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	6.07	pKi	>854	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
GtoPdb	-	-	6.07	pKi	>854	nM	Ki	ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	Uptake Assay Protocol: NET: This protocol was designed to measure inhibition of uptake by the human norepinephrine transporter. The reagents were human NET (HEK293F) cells, desipramine (Sigma), nomifensine, neurotransmitter transporter uptake assay kit (Molecular Devices), freestyle 293 expression medium (Invitrogen), 10× Hank's Balanced Salt Solution (HBSS; Invitrogen), 1 M HEPES (Mediatech), Biocoat poly-D-lysine 96-well, black, clear plates (Becton, Dickinson), and 500 μL polypropylene U-bottom 96-well plates (Fisher). The Assay Buffer (AB) was 1×HBSS and 0.02 M HEPES.The HEK293F cells were transfected with the human norepinephrine transporter and frozen in 1 mL aliquots at about 1E+07 cells/mL. On the day of the experiment, the cells were removed from −80° C. or liquid nitrogen and thawed in a room temperature water bath. The cells were dilute to about 1-2E+06 with Freestyle medium. A 1 mL sample (1:2 dilution) was prepared, and the cells were counted. The cells were spun at 1100 rpm for 5 minutes, and the medium was aspirated off. The cells were resuspend in medium at 1.5E+06 cells/mL for about 60,000 cells per well. 40 μL of cells were dispensed per well in the Biocoat plates. The plates were spun at 1100 rpm for 1 minute to improve homogeneity of the cell layer and were incubated at 37° C. for a minimum of 3 hours.	B	6.18	pKi	668	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	6.19	pKi	>650	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
GtoPdb	-	-	6.19	pKi	>650	nM	Ki	ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
ChEMBL	Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	5.82	pIC50	1500	nM	IC50	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Inhibition of human NET expressed in CHO cells assessed as reduction of [3H]-NE re-uptake preincubated for 10 mins followed by [3H]-NE addition measured after 10 mins by liquid scintillation counting	B	6.27	pIC50	538	nM	IC50	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb	-	-	7.82	pKi	15	nM	Ki	ACS Med Chem Lett (2013) 4: 560-4 [PMID:24900709]
ChEMBL	Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	7.82	pKi	15	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Uptake Assay Protocol: SERT: This protocol was designed to measure inhibition of uptake by the human serotonin transporter. The reagents were human SERT (HEK293F) cells, fluoxetine (Sigma), nomifensine, neurotransmitter transporter uptake assay kit (Molecular Devices), freestyle 293 expression medium (Invitrogen), 10× Hank's Balanced Salt Solution (HBSS; Invitrogen), 1 M HEPES (Mediatech), Biocoat poly-D-lysine 96-well, black, clear plates (Becton, Dickinson), and 500 μL polypropylene U-bottom 96-well plates (Fisher). The Assay Buffer (AB) was 1λ HBSS and 0.02 M HEPES.The HEK293F cells were transfected with the human serotonin transporter and frozen in 1 mL aliquots at about 1E+07 cells/mL. On the day of the experiment, the cells were removed from −80° C. or liquid nitrogen and thawed in a room temperature water bath. The cells were dilute to about 1-2E+06 with Freestyle medium. A 1 mL sample (1:2 dilution) was prepared, and the cells were counted. The cells were spun at 1100 rpm for 5 minutes, and the medium was aspirated off. The cells were resuspend in medium at 1.5E+06 cells/mL for about 60,000 cells per well. 40 μL of cells were dispensed per well in the Biocoat plates. The plates were spun at 1100 rpm for 1 minute to improve homogeneity of the cell layer and were incubated at 37° C. for a minimum of 3 hours.	B	8.39	pKi	4.1	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Inhibition of human SERT expressed in CHO cells assessed as reduction of [3H]-5-HT re-uptake preincubated for 10 mins followed by [3H]-5-HT addition measured after 10 mins by liquid scintillation counting	B	7.28	pIC50	53	nM	IC50	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL	Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	7.77	pIC50	17	nM	IC50	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr	B	6.49	pKi	>324	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes	F	6.74	pIC50	180	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]

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]