ChEMBL ligand: CHEMBL637 (Alventa xl, Amphero xl, Bonilux xl, Depefex xl, Efectin, Efexor, Efexor xl, Effexor, Foraven xl, Kanghong, Mentaven xl, NSC-758676, Politid xl, Ranfaxine xl, Rodomel xl, Sunveniz xl, Tardcaps xl, Tifaxin xl, Tonpular xl, Trevilor, Trixat xl, Vaxalin xl, Velafax, Venaxx xl, Venlablue xl, Venladex xl, Venlafaxina, Venlafaxine, Venlalic xl, Venlaneo xl, Venlor, Vensir xl, Vexarin xl, Viepax, Viepax xl, Winfex xl)
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!
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] DAT/Dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] 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	6.85	pIC50	140	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain	B	6.96	pIC50	109	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of binding of [3H]imipramine to imipramine receptor in rat brain	B	7.05	pIC50	90	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	Equilibrium dissociation constant (KD) for Competitive binding between [3H]WIN-35428 and the compound at human transporter-hDAT	B	5.03	pKd	9300	nM	Kd	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	Binding affinity to human DAT expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting	B	5.28	pKi	5300	nM	Ki	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	5.44	pKi	3620	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	6.05	pKi	>890	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Inhibition of DA reuptake at human DAT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	B	4.8	pIC50	15767	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340]
ChEMBL	Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	5.04	pIC50	9120.11	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of dopamine reuptake at human dopamine transporter expressed in CHO cells	B	5.13	pIC50	7340	nM	IC50	Bioorg Med Chem Lett (2010) 20: 5567-5571 [PMID:20724153]
ChEMBL	Inhibition of DAT	B	5.35	pIC50	4430	nM	IC50	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Inhibition of human DAT expressed in CHOK1 cells assessed as decrease in [3H]-dopamine reuptake after 10 mins by scintillation counting method	B	5.35	pIC50	4430	nM	IC50	J Med Chem (2018) 61: 3779-3798 [PMID:29039662]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Inhibition of [3H]- DA reuptake into rat striatal synaptosomes	B	6.44	pKi	360	nM	Ki	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	Inhibition of [3H]dopamine reuptake at rat brain frontal cortex dopamine transporter	B	3	pIC50	>1000000	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1256-1259 [PMID:20022503]
ChEMBL	Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter	B	5.97	pKd	1060	nM	Kd	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.57	pKi	2685	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	5.79	pKi	1623	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	6.26	pKi	>553	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Displacement of [3H]nisoxetine from human norepinephrine transporter expressed in MDCK-Net6 cells	B	6.41	pKi	385	nM	Ki	J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL	Binding affinity to human NET expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting	B	6.68	pKi	210	nM	Ki	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL	Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	5.1	pIC50	7943.28	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	B	5.24	pIC50	5722	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.57	pIC50	2708	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]Nisoxetine from human NET transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	6.17	pIC50	680	nM	IC50	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells	B	6.24	pIC50	581	nM	IC50	Bioorg Med Chem Lett (2010) 20: 5567-5571 [PMID:20724153]
GtoPdb	-	-	6.27	pIC50	535	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-12 [PMID:20378347]
ChEMBL	Inhibition of human NET transfected in MDCK-Net6 cells	B	6.27	pIC50	535	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347]
ChEMBL	Inhibition of norepinephrine uptake at human norepinephrine transporter expressed in MDCK-Net6 cells	B	6.27	pIC50	535	nM	IC50	J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL	Inhibition of human NET expressed in MDCK cells assessed as decrease in [3H]-noradrenaline reuptake after 10 mins by scintillation counting method	B	6.83	pIC50	149	nM	IC50	J Med Chem (2018) 61: 3779-3798 [PMID:29039662]
ChEMBL	Inhibition of NET	B	6.83	pIC50	149	nM	IC50	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats	B	6.14	pKi	719	nM	Ki	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
ChEMBL	Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes	B	6.86	pKi	138	nM	Ki	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes	F	5.5	pIC50	3140	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes	F	6.12	pIC50	760	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes	F	6.19	pIC50	640	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity against 5-hydroxytryptamine 1A receptor (5-HT1A) by displacement of [3H]8-OH-DPAT from rat hippocampus membranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL	Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Equilibrium dissociation constant (KD) for Competitive binding between [3H]- imipramine and the compound at human transporter-hSERT	B	8.05	pKd	8.9	nM	Kd	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	6.95	pKi	113	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Binding affinity to human SERT expressed in HEK293 cells after 60 mins in presence of [3H]imipramine by liquid scintillation counting	B	7.41	pKi	39	nM	Ki	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	7.96	pKi	11	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	8.42	pKi	3.81	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Inhibition of [3H]5-HT uptake at human SERT expressed in HEK293 cells preincubated for 10 mins prior to substrate addition measured after 4 mins by FLIPR assay	B	6.49	pIC50	323.59	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay	B	7.44	pIC50	36.1	nM	IC50	Bioorg Med Chem Lett (2014) 24: 3234-3237 [PMID:24974340]
ChEMBL	Inhibition of serotonin reuptake at human SERT expressed in HEK293 cells	B	7.46	pIC50	35	nM	IC50	Bioorg Med Chem Lett (2010) 20: 5567-5571 [PMID:20724153]
ChEMBL	Inhibition of 5HT uptake at human SERT expressed in human JAR cells	B	7.51	pIC50	31	nM	IC50	J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL	Inhibition of human SERT expressed in human JAR cells	B	7.57	pIC50	27	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347]
GtoPdb	-	-	7.57	pIC50	27	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-12 [PMID:20378347]
ChEMBL	Inhibition of human SERT expressed in HEK293 cells assessed as decrease in [3H]-serotonin reuptake after 10 mins by scintillation counting method	B	7.7	pIC50	20	nM	IC50	J Med Chem (2018) 61: 3779-3798 [PMID:29039662]
ChEMBL	Inhibition of SERT	B	7.7	pIC50	20	nM	IC50	J Med Chem (2011) 54: 2529-2591 [PMID:21413808]
ChEMBL	Displacement of [3H]citalopram from human SERT transfected in HEK293 cells after 3 hrs by Wallac counting analysis	B	7.7	pIC50	>20	nM	IC50	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	8.14	pIC50	7.18	nM	IC50	DrugMatrix in vitro pharmacology data
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats	B	7.28	pKi	52	nM	Ki	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
ChEMBL	Inhibition of [3H]5-HT reuptake into rat frontal cortex synaptosomes	B	7.43	pKi	37	nM	Ki	Bioorg Med Chem Lett (1998) 8: 487-492 [PMID:9871604]
ChEMBL	Displacement of [3H]-citalopram from Sprague-Dawley rat brain SERT after 1 hr	B	7.6	pKi	25	nM	Ki	ACS Med Chem Lett (2013) 4: 560-564 [PMID:24900709]
ChEMBL	Inhibition of [3H]5HT reuptake at rat brain frontal cortex serotonin transporter	B	6.46	pIC50	350	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1256-1259 [PMID:20022503]
ChEMBL	Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes	F	6.68	pIC50	210	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of 5HT uptake at rat brain SERT	B	6.68	pIC50	210	nM	IC50	J Med Chem (2008) 51: 4038-4049 [PMID:18557608]
ChEMBL	Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes	F	6.72	pIC50	190	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
ChEMBL	Inhibition of uptake of tritiated serotonin (5-HT) into rat brain synaptosomes	F	7	pIC50	100	nM	IC50	J Med Chem (1990) 33: 2899-2905 [PMID:1976813]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Inhibition of [3H]norepinephrine reuptake at rat brain frontal cortex norepinephrine transporter	B	5.85	pIC50	1400	nM	IC50	Bioorg Med Chem Lett (2010) 20: 1256-1259 [PMID:20022503]
ChEMBL	Inhibition of norepinephrine uptake at rat brain norepinephrine transporter	B	6.19	pIC50	640	nM	IC50	J Med Chem (2008) 51: 4038-4049 [PMID:18557608]

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]