ChEMBL ligand: CHEMBL281594 (GBR 12909, GBR-12909, Vanoxerine)
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] DAT/Dopamine transporter in Mouse [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327] 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!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Mouse [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
Sigma-1 receptor in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] 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!
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
DAT/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	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	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]
ChEMBL	Displacement of [125I]RTI55 from DAT	B	8.43	pKi	3.7	nM	Ki	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
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/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/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/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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 [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]
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]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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/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/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
Sigma-1 receptor 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]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor 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 opioid receptor 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]
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]
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 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]