ChEMBL ligand: CHEMBL281594 (GBR 12909, GBR-12909, Vanoxerina, Vanoxerine)
Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] Sigma non-opioid intracellular receptor 1 in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] 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] DAT/Sodium-dependent dopamine transporter in Mouse [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327] DAT/Sodium-dependent dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] 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 Mouse [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] 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!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] There should be some charts here, you may need to enable JavaScript!
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
σ2 in Rat [GtoPdb: 2553] [UniProtKB: Q5U3Y7] 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
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	In vitro binding affinity towards Norepinephrine transporter rat cerebral cortical homogenates by [3H]nisoxetine displacement.	B	4.7	pKi	>20000	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Binding affinity at norepinephrine transporter using [3H]nisoxetine as radioligand from rat brain	B	5.9	pKi	1270	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867]
ChEMBL	Displacement of [3H]nisoxetine from rat brain norepinephrine transporter	B	5.9	pKi	1270	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
ChEMBL	The compound was tested for binding affinity nisoxatine ligand	B	5.9	pKi	1270	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Inhibition of [3H]NE uptake in NET in rat cerebral cortex	B	6.99	pKi	102	nM	Ki	Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549]
ChEMBL	Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]-NE	F	6.99	pKi	102	nM	Ki	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	Inhibition of NET-mediated [3H]NE uptake in rat cerebral cortex	B	6.99	pKi	102	nM	Ki	J Med Chem (2006) 49: 4239-4247 [PMID:16821783]
ChEMBL	Inhibition of [3H]norepinephrine uptake at the rat norepinephrine transporter.	B	7.1	pKi	79	nM	Ki	J Med Chem (2003) 46: 1465-1469 [PMID:12672246]
ChEMBL	Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement.	B	6.3	pIC50	496	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum	B	6.3	pIC50	496	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762]
ChEMBL	Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex.	B	6.3	pIC50	496	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand	B	6.3	pIC50	496	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand	B	6.3	pIC50	496	nM	IC50	J Med Chem (2001) 44: 937-948 [PMID:11300876]
ChEMBL	Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]NE	F	6.94	pIC50	114	nM	IC50	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand	B	6.5	pKi	318	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
ChEMBL	Sigma receptor binding was determined by labeling with radioligand [3H](+)-pentazocine on frozen membranes obtained from frozen guinea pig brain	B	7.37	pIC50	43	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	The compound was tested for affinity towards sigma-3 receptor	B	9	pIC50	1	nM	IC50	J Med Chem (1994) 37: 4109-4117 [PMID:7990111]
sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL	Binding affinity of Sigma opioid receptor type 2 in rat liver membranes using [3H]DTG ligand	B	6.94	pKi	116	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
GtoPdb	-	-	7.32	pIC50	48	nM	IC50	Life Sci (1990) 47: PL133-7 [PMID:1980329]
Sigma non-opioid intracellular receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL	Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane	B	7.29	pKi	50.8	nM	Ki	Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	Displacement of [3H]WIN35428 from DAT after 1.5 hrs by scintillation counting	B	7.66	pKi	22	nM	Ki	Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583]
ChEMBL	Displacement of [3H]-WIN35428 from human DAT expressed in HEK293 cells measured after 30 mins	B	8.06	pKi	8.8	nM	Ki	J Med Chem (2016) 59: 6329-6343 [PMID:27309376]
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	8.06	pKi	8.7	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Inhibition of [3H]dopamine reuptake at dopamine transporter	B	8.29	pKi	5.07	nM	Ki	J Med Chem (2009) 52: 5872-5879 [PMID:19791802]
ChEMBL	Displacement of [3H]-WIN35428 from human DAT expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay	B	8.33	pKi	4.7	nM	Ki	Bioorg Med Chem (2021) 51: 116509-116509 [PMID:34798381]
ChEMBL	Displacement of [125I]RTI55 from DAT	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Binding affinity towards dopamine transporter (DAT) by using [125I]RTI-55 radioligand	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2002) 45: 4371-4374 [PMID:12213078]
GtoPdb	-	-	9	pKi	1	nM	Ki	Eur J Pharmacol (1989) 166: 493-504 [PMID:2530094]; Eur J Pharmacol (1984) 103: 241-8 [PMID:6237922]; J Pharmacol Exp Ther (1991) 258: 626-32 [PMID:1678014]
ChEMBL	Competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with human dopamine transporter	B	9.44	pKi	0.36	nM	Ki	J Med Chem (2000) 43: 639-648 [PMID:10691690]
ChEMBL	Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	B	6.72	pIC50	190	nM	IC50	ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656]
ChEMBL	Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method	B	7.37	pIC50	43	nM	IC50	Bioorg Med Chem (2017) 25: 2266-2276 [PMID:28274674]
ChEMBL	Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells	B	7.37	pIC50	43	nM	IC50	J Med Chem (1998) 41: 3293-3297 [PMID:9703474]
ChEMBL	Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting	B	7.4	pIC50	40	nM	IC50	Bioorg Med Chem (2017) 25: 5278-5289 [PMID:28807575]
ChEMBL	Inhibition of human DAT	B	7.57	pIC50	27	nM	IC50	J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL	Affinity was evaluated using [3H]DA (radioligand) on Cloned human Dopamine transporter expressed in HEK cells	B	7.59	pIC50	26	nM	IC50	J Med Chem (1998) 41: 3293-3297 [PMID:9703474]
ChEMBL	Inhibition of human dopamine transporter	B	8.14	pIC50	7.2	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	The inhibition of reuptake against dopamine transporter	F	8.37	pIC50	4.3	nM	IC50	J Med Chem (2002) 45: 4371-4374 [PMID:12213078]
DAT/Sodium-dependent dopamine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327]
ChEMBL	Displacement of [3H]RTI-121 from mouse DAT in striatal membranes	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem (2015) 23: 222-230 [PMID:25468036]
DAT/Sodium-dependent dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Inhibition of [3H]DA uptake at DAT in rat brain striatal synaptosomes by liquid scintillation spectrophotometry	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131]
ChEMBL	Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand	B	7.92	pKi	12.02	nM	Ki	J Med Chem (2000) 43: 4151-4159 [PMID:11063611]
ChEMBL	Binding affinity at dopamine transporter from rat caudate-putamen tissue by [3H]WIN-35428 displacement.	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem Lett (2003) 13: 629-632 [PMID:12639545]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue	B	7.92	pKi	12	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2387-2390 [PMID:12161139]
ChEMBL	Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand	B	7.92	pKi	12	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain	B	7.92	pKi	11.9	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
ChEMBL	Binding affinity at Dopamine transporter by displacing [3H]WIN-35428 from rat caudate putamen	B	7.92	pKi	11.9	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867]
ChEMBL	Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen	B	7.94	pKi	11.6	nM	Ki	J Med Chem (1994) 37: 2258-2261 [PMID:8057273]
ChEMBL	Affinity for rat dopamine transporter using [3H]WIN-35428 displacement.	B	7.94	pKi	11.6	nM	Ki	J Med Chem (1995) 38: 3933-3940 [PMID:7562926]
ChEMBL	Inhibition of DAT-mediated [3H]DA uptake in rat striatum	B	7.97	pKi	10.6	nM	Ki	J Med Chem (2006) 49: 4239-4247 [PMID:16821783]
ChEMBL	Inhibition of rat brain dopamine transporter as accumulation of [3H]DA	F	7.97	pKi	10.6	nM	Ki	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	Inhibition of [3H]dopamine uptake in DAT in rat striatum	B	7.97	pKi	10.6	nM	Ki	Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549]
ChEMBL	Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL	Displacement of [3H]WIN-from DAT in rat striatum	B	7.99	pKi	10.2	nM	Ki	Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat striatum DAT	B	8.07	pKi	8.56	nM	Ki	J Med Chem (2006) 49: 4239-4247 [PMID:16821783]
ChEMBL	Inhibition of [3H]dopamine uptake via rat dopamine receptor.	B	8.37	pKi	4.3	nM	Ki	J Med Chem (2003) 46: 1465-1469 [PMID:12672246]
ChEMBL	Binding affinity against dopamine transporter labelled with [125I]- RTI-55 in rat.	B	8.43	pKi	3.7	nM	Ki	J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL	Binding affinity for dopamine transporter	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2002) 45: 1321-1329 [PMID:11882001]
ChEMBL	Displacement of [125I]RTI55 from DAT in rat brain synaptosomes	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem (2007) 15: 1146-1159 [PMID:17127069]
ChEMBL	Affinity at rat dopamine transporter using [125I]RTI-55 displacement.	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2003) 46: 1465-1469 [PMID:12672246]
ChEMBL	Binding affinity against Dopamine transporter using [125]RTI-55	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2001) 44: 3937-3945 [PMID:11689080]
ChEMBL	Binding affinity towards dopamine transporter (DAT)	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288]
ChEMBL	Displacement of [3H]WIN-35428 from DAT in rat striatum membrane	B	8.75	pKi	1.77	nM	Ki	Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292]
ChEMBL	Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes	B	9.06	pKi	0.88	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL	In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement.	B	10.22	pKi	0.06	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]-5-HT on synaptosomes obtained from whole rat brain minus cerebellum.	F	7.14	pIC50	73	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Inhibition of [3H]cocaine binding to the dopamine transporter.	B	7.44	pIC50	36	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the dopamine transporter.	B	7.48	pIC50	33	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter.	B	7.62	pIC50	24	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum	B	7.68	pIC50	21.1	nM	IC50	J Med Chem (2004) 47: 6128-6136 [PMID:15566284]
ChEMBL	IC50 value was evaluated using [3H]WIN-35428 (radioligand) on Dopamine transporter in rat striatum.	B	7.71	pIC50	19.3	nM	IC50	J Med Chem (1998) 41: 3293-3297 [PMID:9703474]
ChEMBL	Inhibition of rat brain Dopamine transporter uptake as [3H]DA accumulation	F	7.85	pIC50	14.2	nM	IC50	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	Inhibitory activity against dopamine transporter (DAT) labeled with [3H]WIN-35428 in rat brain striatal membrane.	B	7.85	pIC50	14	nM	IC50	J Med Chem (1998) 41: 699-705 [PMID:9513598]
ChEMBL	In vitro inhibition of [3H]WIN-35 428 binding to dopamine transporter on rat striatal membranes.	B	7.85	pIC50	14	nM	IC50	J Med Chem (1997) 40: 35-43 [PMID:9016326]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat brain dopamine transporter	B	7.97	pIC50	10.6	nM	IC50	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum.	B	7.97	pIC50	10.6	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum	B	7.97	pIC50	10.6	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762]
ChEMBL	Binding affinity towards dopamine transporter in rat striatum using [3H]WIN-35 428 as radioligand	B	7.97	pIC50	10.6	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement.	B	7.97	pIC50	10.6	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement.	B	7.97	pIC50	10.6	nM	IC50	J Med Chem (2001) 44: 937-948 [PMID:11300876]
ChEMBL	Reuptake inhibition of [3H]-labeled dopamine (DA) in rat.	F	8.14	pIC50	7.3	nM	IC50	J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL	Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]dopamine on synaptosomes obtained from rat caudate.	F	8.14	pIC50	7.3	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Inhibition of [3H]DA reuptake in rat caudate homogenate.	F	8.14	pIC50	7.3	nM	IC50	J Med Chem (2000) 43: 4840-4849 [PMID:11123994]
ChEMBL	Inhibition of uptake from dopamine transporter in rat striatum using [3H]DA as radioligand	F	8.18	pIC50	6.63	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Binding affinity at dopamine transporter from rat striatal membrane tissue by [3H]CFT displacement.	B	8.22	pIC50	6	nM	IC50	J Med Chem (1996) 39: 749-756 [PMID:8576918]
ChEMBL	Binding against Dopamine transporter using radioligand as [3H]GBR 12935	B	8.26	pIC50	5.5	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Inhibition of dopamine DA reuptake	B	8.37	pIC50	4.3	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Compound was tested for its ability to inhibit the uptake of [3H]dopamine in DAT (dopamine transporter system) expressing cell line	F	8.37	pIC50	4.3	nM	IC50	Bioorg Med Chem Lett (1998) 8: 261-266 [PMID:9871666]
ChEMBL	Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand	B	8.37	pIC50	4.3	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL	Inhibition of [3H]BTCP binding to the dopamine transporter.	B	8.4	pIC50	4	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Binding affinity for rat Dopamine transporter.	B	8.43	pIC50	3.7	nM	IC50	J Med Chem (2000) 43: 4840-4849 [PMID:11123994]
ChEMBL	Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55	B	8.43	pIC50	3.7	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Inhibition of [3H]GBR-12935 binding to the dopamine transporter.	B	8.52	pIC50	3	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55 in nonstandard conditions	F	8.58	pIC50	2.63	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Reuptake inhibition was determined at the dopamine transporter labeled with radioligand [3H]dopamine in nonstandard conditions on brain membranes obtained from rat	F	8.76	pIC50	1.75	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.	B	9	pIC50	1	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane	B	9.37	pIC50	0.43	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4915-4918 [PMID:16165350]
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	6.86	pKi	138	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	B	5.84	pIC50	1460	nM	IC50	ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656]
ChEMBL	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 1745860)	F	6.1	pIC50	790	nM	IC50	Sci Rep (2021) 11: 12290-null [PMID:34112854]
ChEMBL	Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method	B	6.96	pIC50	110	nM	IC50	Bioorg Med Chem (2017) 25: 2266-2276 [PMID:28274674]
ChEMBL	Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting	B	6.96	pIC50	110	nM	IC50	Bioorg Med Chem (2017) 25: 5278-5289 [PMID:28807575]
ChEMBL	Compound was tested for the inhibition of norepinephrine (NE) reuptake	F	7.1	pIC50	79	nM	IC50	J Med Chem (2002) 45: 4371-4374 [PMID:12213078]
SERT/Sodium-dependent serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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	6.77	pKi	168	nM	Ki	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
ChEMBL	Displacement of [125I]RTI55 from SERT	B	6.89	pKi	130	nM	Ki	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Binding affinity for serotonin transporter (SERT) using [125I]RTI-55	B	6.9	pKi	126	nM	Ki	J Med Chem (2002) 45: 4371-4374 [PMID:12213078]
ChEMBL	Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay	B	5.42	pIC50	3840	nM	IC50	ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656]
ChEMBL	Affinity was evaluated using [3H]citalopram (radioligand) on human serotonin transporter expressed in HEK cells	B	6.13	pIC50	741	nM	IC50	J Med Chem (1998) 41: 3293-3297 [PMID:9703474]
ChEMBL	The inhibition of reuptake against Serotonin transporter (5-HT)	F	7.14	pIC50	73	nM	IC50	J Med Chem (2002) 45: 4371-4374 [PMID:12213078]
SERT/Sodium-dependent serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857]
ChEMBL	Displacement of [3H]paroxetine from mouse SERT in whole brain membrane	B	7.62	pKi	24.1	nM	Ki	Bioorg Med Chem (2015) 23: 222-230 [PMID:25468036]
SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Binding affinity for serotonin transporter	B	6.89	pKi	130	nM	Ki	J Med Chem (2002) 45: 1321-1329 [PMID:11882001]
ChEMBL	Binding affinity against serotonin transporter using [125]RTI-55	B	6.89	pKi	130	nM	Ki	J Med Chem (2001) 44: 3937-3945 [PMID:11689080]
ChEMBL	Binding affinity against Serotonin transporter (SERT) labelled with [125I]RTI-55 in rat.	B	6.9	pKi	126	nM	Ki	J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL	Displacement of [125I]RTI55 from SERT in rat brain synaptosomes	B	6.9	pKi	126	nM	Ki	Bioorg Med Chem (2007) 15: 1146-1159 [PMID:17127069]
ChEMBL	Binding affinity towards rat serotonin transporter (SERT)	B	6.9	pKi	126	nM	Ki	Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288]
ChEMBL	Affinity at rat serotonin transporter using [125I]RTI-55 displacement.	B	6.9	pKi	126	nM	Ki	J Med Chem (2003) 46: 1465-1469 [PMID:12672246]
ChEMBL	Binding affinity against serotonin transporter by displacement of [3H]citalopram in rat brain	B	6.98	pKi	105	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
ChEMBL	Binding affinity at Serotonin transporter using [3H]citalopram as radioligand from rat brain	B	6.98	pKi	105	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867]
ChEMBL	Displacement of [3H]citalopram from SERT in rat brain stem membrane	B	6.98	pKi	104	nM	Ki	Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292]
ChEMBL	Inhibition of rat brain Serotonin transporter as accumulation of [3H]5-HT	F	7.04	pKi	91.1	nM	Ki	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	Inhibition of SERT-mediated [3H]5-HT uptake in rat cerebral cortex	B	7.04	pKi	91.1	nM	Ki	J Med Chem (2006) 49: 4239-4247 [PMID:16821783]
ChEMBL	Inhibition of [3H]5HT uptake in SERT in rat cerebral cortex	B	7.04	pKi	91.1	nM	Ki	Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549]
ChEMBL	Inhibition of [3H]5-HT uptake at the rat serotonin transporter.	B	7.14	pKi	73	nM	Ki	J Med Chem (2003) 46: 1465-1469 [PMID:12672246]
ChEMBL	In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement.	B	7.28	pKi	52.8	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand	B	7.62	pKi	24.1	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement.	B	6.88	pIC50	132	nM	IC50	J Med Chem (2001) 44: 937-948 [PMID:11300876]
ChEMBL	Inhibition of binding of [3H]- citalopram to Serotonin transporter (SERT) of rat cerebral cortex.	B	6.88	pIC50	132	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum	B	6.88	pIC50	132	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762]
ChEMBL	Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement.	B	6.88	pIC50	132	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand	B	6.88	pIC50	132	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Binding affinity was determined at the Serotonin transporter labeled with radioligand [125 I] RTI-55	B	6.9	pIC50	126	nM	IC50	J Med Chem (1997) 40: 705-716 [PMID:9057857]
ChEMBL	Binding affinity for rat 5-hydroxytryptamine transporter.	B	6.9	pIC50	126	nM	IC50	J Med Chem (2000) 43: 4840-4849 [PMID:11123994]
ChEMBL	Inhibition of rat brain Serotonin transporter uptake as [3H]5-HT accumulation	B	6.99	pIC50	101.4	nM	IC50	J Med Chem (2005) 48: 4962-4971 [PMID:16033275]
ChEMBL	IC50 value was evaluated using [3H]citalopram (radioligand) on serotonin transporter in rat striatum.	B	7.06	pIC50	87	nM	IC50	J Med Chem (1998) 41: 3293-3297 [PMID:9703474]
ChEMBL	Inhibitory activity against serotonin transporter (SERT) labeled with [3H]-citalopram in rat brain striatal membrane.	B	7.06	pIC50	86.6	nM	IC50	J Med Chem (1998) 41: 699-705 [PMID:9513598]
ChEMBL	Binding affinity at serotonin transporter from rat brain striatal membrane by [3H]citalopram displacement.	B	7.09	pIC50	82	nM	IC50	J Med Chem (1996) 39: 749-756 [PMID:8576918]
ChEMBL	In vitro inhibition of [3H]citalopram binding to serotonin transporter on rat striatal membranes.	B	7.09	pIC50	82	nM	IC50	J Med Chem (1997) 40: 35-43 [PMID:9016326]
ChEMBL	Reuptake inhibition of [3H]-5-HT (5-HT) in rat.	F	7.14	pIC50	73	nM	IC50	J Med Chem (1999) 42: 5029-5042 [PMID:10585212]
ChEMBL	Inhibition of [3H]5-HT reuptake at rat serotonin transporter	B	7.14	pIC50	73	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Inhibitory activity against [3H]- 5-hydroxytryptamine reuptake in whole rat brain minus cerebellum	F	7.14	pIC50	73	nM	IC50	J Med Chem (2000) 43: 4840-4849 [PMID:11123994]
ChEMBL	Compound was tested for its ability to inhibit the neurotransmitter serotonin-5-HT reuptake system using [3H]5-HT as radioligand	B	7.15	pIC50	70	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2559-2564
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Displacement of [3H]nisoxetine from NET in rat frontal cortex membrane	B	6.3	pKi	497	nM	Ki	Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	F	6.49	pIC50	320	nM	IC50	J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Activity Assay: HERG: The pre- and post-compound hERG current was evoked by a single voltage pulse consisting of a 20 s period holding at −70 mV, a 160 ms step to −60 mV (to obtain an estimate of leak), a 100 ms step back to −70 mV, a 1 s step to +40 mV, a 2 s step to −30 mV, and finally a 500 ms step to −70 mV. In between the pre- and post-compound voltage pulses, there was no clamping of the membrane potential. Currents were leak-subtracted based on the estimate of current evoked during the +10 mV step at the start of the voltage pulse protocol. The current signal was sampled at 2.5 k Hz. For each compound, the IC50 value was determined.	B	6.33	pIC50	470	nM	IC50	US-9944618-B2. Inhibiting neurotransmitter reuptake (2018)
σ2 in Rat [GtoPdb: 2553] [UniProtKB: Q5U3Y7]
GtoPdb	-	-	7.32	pIC50	48	nM	IC50	Life Sci (1990) 47: PL133-7 [PMID:1980329]

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]