ChEMBL ligand: CHEMBL370805 (Benzoylmethylecgonine, Cocaine, Cocainum, IDS-NC-004, Neurocaine, (r)-(-)-cocaine, RX-0041, RX0041)
Dopamine transporter in Macaca fascicularis [ChEMBL: CHEMBL5032] [UniProtKB: Q9GJT6] DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] Dopamine transporter in Bovine [ChEMBL: CHEMBL2986] [UniProtKB: P27922] 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!
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] 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 Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] 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] 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!
5-HT3AB in Human [GtoPdb: 378] There should be some charts here, you may need to enable JavaScript!
5-HT3A in Human [GtoPdb: 379] 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
Dopamine transporter in Macaca fascicularis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5032] [UniProtKB: Q9GJT6]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine transporter (DAT) of cynomolgus monkey caudate-putamen	B	7.02	pIC50	95.6	nM	IC50	Bioorg Med Chem Lett (1999) 9: 857-862 [PMID:10206550]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	Inhibition of [3H]mazindol binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	5.9	pKi	1270	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [125I]RTI-55 binding to dopamine transporter	B	6.12	pKi	760	nM	Ki	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [125I]RTI-55 binding at Dopamine transporter (DAT) expressed in HEK cells	B	6.12	pKi	759	nM	Ki	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Inhibition of [125I]RTI-55 binding to recombinant human DAT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	6.14	pKi	720	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Displacement of [125I]RTI55 from human DAT expressed in COS1 cell membrane	B	6.2	pKi	630	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
ChEMBL	Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells	B	6.3	pKi	500	nM	Ki	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Displacement of [125I]- RTI-55 from Dopamine transporter expressed in HEK cells	B	6.31	pKi	490	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Displacement of [3H]WIN 35428 from human DAT transiently expressed in COS7 cells	B	6.35	pKi	450	nM	Ki	J Med Chem (2020) 63: 2343-2357 [PMID:31661268]
ChEMBL	Displacement of [125I]RTI-55 from human DAT expressed in HEK293 cells	B	6.36	pKi	432	nM	Ki	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells	B	6.37	pKi	431	nM	Ki	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Displacement of [125I]RT155 binding in HEK cells expressing human DAT	B	6.38	pKi	419	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (low affinity)	B	6.41	pKi	388	nM	Ki	J Med Chem (1996) 39: 1560-1563 [PMID:8691489]
ChEMBL	Displacement of [125I]RTI55 from human recombinant DAT expressed in HEK293 cells	B	6.43	pKi	371	nM	Ki	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Displacement of [125I]RTI55 from human DAT expressed in HEK cells	B	6.43	pKi	371	nM	Ki	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells by scintillation counting	B	6.43	pKi	371	nM	Ki	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	Inhibition of [3H]DA uptake in human DAT expressed in COS1 cell membrane	F	6.46	pKi	347	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
ChEMBL	Binding affinity at DAT	B	6.47	pKi	341	nM	Ki	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Inhibition of reuptake of [3H]DA (20 nM) by dopamine transporter	B	6.48	pKi	330	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Binding affinity against cloned human dopamine transporter using 40-80 pM [125I]RTI.	B	6.52	pKi	300	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Compound was evaluated for inhibition of [3H]DA uptake in HEK-hDAT cells expressing Human dopamine Transporter	B	6.56	pKi	276	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Compound was tested for inhibition of [125I]RTI-55 binding to dopamine transporter in HEK cells	B	6.57	pKi	272	nM	Ki	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Displacement of [125I]RTI55 from cloned human DAT expressed in HEK293 cells	B	6.57	pKi	272	nM	Ki	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Affinity to inhibit [3H]DA uptake	B	6.57	pKi	270	nM	Ki	Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962]
ChEMBL	Compound was evaluated for binding affinity to dopamine transporter using [125I]RTI-55 as a radioligand in HEK cells expressing human transporters.	B	6.59	pKi	258	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
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	6.6	pKi	249	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Ability of compound to inhibit dopamine uptake of receptor was determined	B	6.63	pKi	234.42	nM	Ki	Bioorg Med Chem Lett (2005) 15: 2149-2157 [PMID:15808487]
ChEMBL	Binding Affinity to Dopamine transporter in caudate nuclei which was homogenized and incubated with [3H]mazindol.	B	6.64	pKi	231	nM	Ki	J Med Chem (2000) 43: 351-360 [PMID:10669562]
ChEMBL	Displacement of [3H]WIN35,428 from wild type human DAT expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay	B	6.65	pKi	223	nM	Ki	J Med Chem (2016) 59: 10676-10691 [PMID:27933960]
ChEMBL	Inhibition of DAT (unknown origin) expressed in COS7 cells assessed as reduction in [3H]DA uptake incubated for 5 mins by beta-scintillation counting method	B	6.7	pKi	200	nM	Ki	J Med Chem (2016) 59: 10676-10691 [PMID:27933960]
ChEMBL	Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand from rat caudate putamen tissue (high affinity)	B	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 1560-1563 [PMID:8691489]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT M272L/R344M mutant expressed in HEK293 cells	B	5.93	pIC50	1172	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells	B	5.97	pIC50	1060	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT M272L/1291M/R344M mutant expressed in HEK293 cells	B	6.12	pIC50	759	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Displacement of [3H]WIN35428 from human DAT transfected cell membrane	B	6.17	pIC50	670	nM	IC50	Bioorg Med Chem Lett (2011) 21: 48-51 [PMID:21146984]
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	6.19	pIC50	645.65	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK cells	B	6.23	pIC50	590	nM	IC50	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT R344M mutant expressed in HEK293 cells	B	6.29	pIC50	507	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of [3H]DA uptake in DAT	B	6.32	pIC50	478	nM	IC50	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Inhibition of [3H] dopamine uptake into human DAT expressed in HEK293 cells	F	6.34	pIC50	461	nM	IC50	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Inhibitory activity against [3H]-Dopamine uptake from Dopamine transporter in rat caudate putamen tissue	B	6.39	pIC50	405	nM	IC50	J Med Chem (1996) 39: 1560-1563 [PMID:8691489]
ChEMBL	Displacement of [3H]CFT from human DAT expressed in HEK293 cells	B	6.41	pIC50	392	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Displacement of [125I]-RTI-55 from Dopamine transporter expressed in HEK293 cells	B	6.44	pIC50	367	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Displacement of [3H]CFT from human DAT M272L/R344M mutant expressed in HEK293 cells	B	6.44	pIC50	366	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of [3H]dopamine uptake in HEK cells expressing human DAT	B	6.48	pIC50	330	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	Inhibition of [3H]DA from human recombinant DAT expressed in HEK293 cells	B	6.52	pIC50	303	nM	IC50	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Displacement of [3H]dopamine from human recombinant DAT expressed in HEK293 cells by scintillation counting	B	6.52	pIC50	303	nM	IC50	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	Inhibition of [3H]dopamine uptake in HEK cells expressing human Dopamine transporter	B	6.52	pIC50	301	nM	IC50	Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458]
ChEMBL	Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT)	F	6.53	pIC50	296	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [3H]dopamine uptake in HEK293 cells expressing human dopamine transporter	F	6.54	pIC50	289	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Displacement of [3H]CFT from human DAT R344M mutant expressed in HEK293 cells	B	6.55	pIC50	283	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of recombinant human DAT expressed in HEK293 cell membranes assessed as reduction in [3H]-DA uptake incubated for 22 mins by micro beta scintillation counting analysis	B	6.56	pIC50	274	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells	B	6.57	pIC50	267	nM	IC50	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Compound was tested for inhibition of [3H]DA binding to Dopamine transporter in HEK cells	B	6.57	pIC50	267	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Displacement of [3H]CFT from human DAT M272L/1291M/R344M mutant expressed in HEK293 cells	B	6.59	pIC50	259	nM	IC50	J Biol Chem (2007) 282: 8915-8925 [PMID:17255098]
ChEMBL	Inhibition of [3H]DA uptake at human DAT expressing HEK293 cells	B	6.62	pIC50	240	nM	IC50	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Inhibition of [3H]DA reuptake at human DAT expressed in HEK293 cells	B	6.64	pIC50	227	nM	IC50	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter	B	6.72	pIC50	190	nM	IC50	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [3H]DA uptake in HEK cells expressing dopamine transporter	F	6.72	pIC50	190	nM	IC50	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells	B	6.89	pIC50	130	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL	Inhibition of [3H]3-beta-(4-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to dopamine transporter of cynomolgus monkey striatum	B	7.02	pIC50	95.6	nM	IC50	J Med Chem (1993) 36: 855-862 [PMID:8464040]
ChEMBL	Displacement of [3H]WIN-35428 from human DAT	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2006) 49: 4589-4594 [PMID:16854064]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter	B	7.05	pIC50	89.1	nM	IC50	Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164]
ChEMBL	Displacement of [3H]WIN-35428 from DAT	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2005) 48: 7437-7444 [PMID:16279803]
ChEMBL	Displacement of [3H]WIN-35428 from DAT	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2004) 47: 6401-6409 [PMID:15566309]
ChEMBL	Displacement of [3H]WIN-35428 from DAT	B	7.05	pIC50	89.1	nM	IC50	Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837]
Dopamine transporter in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2986] [UniProtKB: P27922]
ChEMBL	Competitive inhibition against [3H]cocaine binding to cocaine receptor in bovine striatal tissue	B	6.86	pIC50	139	nM	IC50	J Med Chem (1990) 33: 2024-2028 [PMID:2362282]
ChEMBL	In vitro inhibitory activity towards [3H]cocaine binding to rat striatal tissue	B	7.19	pIC50	65	nM	IC50	J Med Chem (1991) 34: 702-705 [PMID:1995895]
DAT/Dopamine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327]
ChEMBL	Inhibition of [125I]RTI-55 binding to mouse DAT expressed in HEK293 cells preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	6.07	pKi	850	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of mouse DAT expressed in HEK293 cells assessed as reduction in [3H]-DA uptake	B	6.7	pIC50	200	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat dopamine transporter	B	4.49	pKi	32000	nM	Ki	J Med Chem (2005) 48: 1336-1343 [PMID:15743177]
ChEMBL	Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes	B	6.19	pKi	642	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL	Binding affinity for dopamine transporters in rat brain tissue.	B	6.29	pKi	510	nM	Ki	J Med Chem (1994) 37: 1558-1561 [PMID:8201589]
ChEMBL	Displacement of [125I]RTI-55 from Dopamine transporter of rat caudate membranes	B	6.34	pKi	460	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2225-2228 [PMID:12127543]
ChEMBL	Ability to inhibit reuptake of dopamine ([3H]DA) at dopamine transporter of rat striatum	B	6.37	pKi	423	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL	Ability to inhibit [3H]DA reuptake at dopamine transporter from rat brain	B	6.37	pKi	423	nM	Ki	J Med Chem (2003) 46: 1997-2007 [PMID:12723962]
ChEMBL	Inhibition of high affinity uptake by the dopamine transporter from rat synaptosomal nerve endings by using [3H]DA as radioligand	B	6.37	pKi	423	nM	Ki	J Med Chem (2004) 47: 5821-5824 [PMID:15537337]
ChEMBL	Inhibition of [3H]DA uptake by dopamine transporter of rat striata synaptosomes	B	6.37	pKi	423	nM	Ki	J Med Chem (2000) 43: 1215-1222 [PMID:10737754]
ChEMBL	Inhibition of high affinity DA uptake into rat synaptosomes using [3H]DA	B	6.37	pKi	423	nM	Ki	J Med Chem (2001) 44: 1615-1622 [PMID:11334571]
ChEMBL	Ability to inhibit high affinity reuptake of [3H]DA from dopamine transporter into nerve endings synaptosomes	B	6.37	pKi	423	nM	Ki	J Med Chem (2002) 45: 1930-1941 [PMID:11960503]
ChEMBL	Binding affinity for [3H]DA (Dopamine transporter) uptake by striated synaptosomes	B	6.37	pKi	423	nM	Ki	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Inhibition of high affinity uptake of [3H]dopamine into nerve endings (synaptosomes) prepared from various regions of the rat brain.	B	6.37	pKi	423	nM	Ki	J Med Chem (2000) 43: 3283-3294 [PMID:10966747]
ChEMBL	Inhibition of reuptake of [3H]DA at Dopamine transporter (DAT)	B	6.37	pKi	423	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Compound was tested for its ability to inhibit high affinity uptake of [3H]DA into rat striatal membrane	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328]
ChEMBL	Inhibition of [3H]dopamine uptake at striatal nerve endings by dopamine transporter	B	6.38	pKi	420	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593]
ChEMBL	Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue	B	6.41	pKi	390	nM	Ki	J Med Chem (1998) 41: 2430-2435 [PMID:9632375]
ChEMBL	Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand.	B	6.41	pKi	390	nM	Ki	J Med Chem (1996) 39: 4744-4749 [PMID:8941387]
ChEMBL	Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue	B	6.41	pKi	388	nM	Ki	J Med Chem (1994) 37: 3875-3877 [PMID:7966147]
ChEMBL	Displacement of [3H]WIN-35428 binding to the dopamine transporter (DAT) in Rat Caudate Putamen	B	6.41	pKi	388	nM	Ki	J Med Chem (1997) 40: 851-857 [PMID:9083473]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen	B	6.41	pKi	388	nM	Ki	J Med Chem (1997) 40: 858-863 [PMID:9083474]
ChEMBL	Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen	B	6.41	pKi	388	nM	Ki	J Med Chem (1994) 37: 2258-2261 [PMID:8057273]
ChEMBL	In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement.	B	6.46	pKi	350	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Inhibition of high affinity uptake of [3H]dopamine into striatal nerve endings (synaptosomes)	B	6.49	pKi	320	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1831-1836 [PMID:10406650]
ChEMBL	Inhibition of [3H]DA binding to dopamine transporter of rat brain synaptosomes	B	6.52	pKi	301	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724]
ChEMBL	Binding affinity at dopamine transporter in rat brain by [3H]WIN-35428 displacement.	B	6.55	pKi	285	nM	Ki	J Med Chem (2004) 47: 3388-3398 [PMID:15189035]
ChEMBL	In vitro dopamine transporter binding affinity using [3H]WIN-35428 as radioligand was determined	B	6.55	pKi	285	nM	Ki	J Med Chem (2003) 46: 2908-2916 [PMID:12825932]
ChEMBL	Binding affinity of compound on dopamine transporters of rat striated membranes using [3H]- mazindol.	B	6.55	pKi	281	nM	Ki	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Binding affinity to inhibit [3H]mazindol binding in rat corpus striatum P2 synaptosomes	B	6.55	pKi	280	nM	Ki	Bioorg Med Chem Lett (1994) 4: 303-308
ChEMBL	Binding affinity was tested by measuring its ability to displace [3H]mazindol binding against dopamine transporter (DAT) of rat striatal membranes	B	6.55	pKi	280	nM	Ki	J Med Chem (1994) 37: 3440-3442 [PMID:7932572]
ChEMBL	ability to displace [3H]- Mazindol binding to cocaine binding sites on Dopamine transporter of rat striatal membranes	B	6.55	pKi	280	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328]
ChEMBL	Binding affinity towards dopamine transporter using [3H]- mazindol as radioligand in rat striatal membranes	B	6.55	pKi	280	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1831-1836 [PMID:10406650]
ChEMBL	Inhibition of [3H]DA Uptake was measured by liquid scintillation spectrometry	B	6.56	pKi	274	nM	Ki	J Med Chem (2000) 43: 351-360 [PMID:10669562]
ChEMBL	Inhibition of [3H]DA uptake at Dopamine transporter in rat cortex.	B	6.57	pKi	270	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356]
ChEMBL	Inhibition of [3H]DA reuptake at dopamine transporter in rat striatum	B	6.59	pKi	259	nM	Ki	Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701]
ChEMBL	Inhibition of high affinity uptake of [3H]DA using rat nerve endings obtained from brain regions enriched in DAT.	B	6.59	pKi	259	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143]
ChEMBL	Inhibition of high affinity uptake of [3H]-DA by dopamine transporter in nerve endings obtained from rat brain.	B	6.59	pKi	259	nM	Ki	J Med Chem (2002) 45: 3161-3170 [PMID:12109901]
ChEMBL	Ability to inhibit high affinity uptake of [3H]DA at Dopamine transporter (DAT) using rat brain striatum	B	6.59	pKi	259	nM	Ki	J Med Chem (2004) 47: 3009-3018 [PMID:15163183]
ChEMBL	Inhibition of [3H]DA uptake by rat striatal dopamine transporter	B	6.62	pKi	241.3	nM	Ki	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Displacement of [3H]WIN-35428 from DAT in rat brain	B	6.63	pKi	237	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846]
ChEMBL	Displacement of [3H]mazindol from cocaine binding site on Dopamine transporter (DAT)	B	6.64	pKi	230	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593]
ChEMBL	Displacement of [3H]mazindol binding to dopamine transporter (DAT) in rat synaptosomes	B	6.64	pKi	230	nM	Ki	J Med Chem (2001) 44: 1615-1622 [PMID:11334571]
ChEMBL	Inhibition of [3H]mazindol binding to dopamine transporter of rat striatal membranes.	B	6.64	pKi	230	nM	Ki	J Med Chem (2000) 43: 3283-3294 [PMID:10966747]
ChEMBL	Inhibition of [3H]- Mazindol binding to dopamine transporter of rat striatal membrane.	B	6.64	pKi	230	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue	B	6.73	pKi	187	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2387-2390 [PMID:12161139]
ChEMBL	Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand	B	6.73	pKi	187	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	6.73	pKi	187	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
ChEMBL	Displacement of [3H]WIN-35248 from dopamine transporter (DAT) of rat striatal membrane	B	6.84	pKi	146	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143]
ChEMBL	Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat striatum synaptosome	B	6.95	pKi	111	nM	Ki	Bioorg Med Chem (2007) 15: 3748-3755 [PMID:17399987]
ChEMBL	Displacement of [3H]GBR-12935 from dopamine transporter of rat caudate-putamen	B	7.05	pKi	89	nM	Ki	Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL	Displacement of [3H]WIN-from DAT in rat brain membrane	B	7.13	pKi	74.3	nM	Ki	Bioorg Med Chem Lett (2005) 15: 5419-5423 [PMID:16213721]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter of rat brain membrane	B	7.13	pKi	74.3	nM	Ki	Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693]
ChEMBL	Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat brain membranes	B	7.14	pKi	71.8	nM	Ki	ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069]
ChEMBL	Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat brain	B	7.14	pKi	71.8	nM	Ki	J Med Chem (2006) 49: 6391-6399 [PMID:17034144]
ChEMBL	Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue	B	7.49	pKi	32	nM	Ki	J Med Chem (1998) 41: 2430-2435 [PMID:9632375]
ChEMBL	Binding affinity against dopamine transporter in rat caudate putamen tissue using [3H]WIN-35428 radioligand. (from other reference)	B	7.49	pKi	32	nM	Ki	J Med Chem (1996) 39: 4744-4749 [PMID:8941387]
ChEMBL	Affinity for rat dopamine transporter using [3H]WIN-35428 displacement.	B	7.49	pKi	32	nM	Ki	J Med Chem (1995) 38: 3933-3940 [PMID:7562926]
ChEMBL	Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue	B	7.49	pKi	32	nM	Ki	J Med Chem (1994) 37: 3875-3877 [PMID:7966147]
ChEMBL	Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue	B	7.49	pKi	32	nM	Ki	J Med Chem (2002) 45: 1203-1210 [PMID:11881989]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter (DAT) in Rat Caudate Putamen	B	7.49	pKi	32	nM	Ki	J Med Chem (1997) 40: 858-863 [PMID:9083474]
ChEMBL	Displacement of [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue	B	7.49	pKi	32	nM	Ki	J Med Chem (1997) 40: 4406-4414 [PMID:9435910]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal membranes.	B	4.8	pIC50	15800	nM	IC50	J Med Chem (1993) 36: 3572-3579 [PMID:8246225]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter	B	4.8	pIC50	15800	nM	IC50	J Med Chem (1991) 34: 883-886 [PMID:2002468]
ChEMBL	Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter.	B	5.74	pIC50	1810	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]GBR-12935 binding to the dopamine transporter.	B	5.84	pIC50	1450	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]dopamine uptake at the dopamine transporter.	B	6.07	pIC50	843	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Binding against Dopamine transporter using radioligand as [3H]GBR 12935	B	6.18	pIC50	660	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Compound was evaluated for its ability to displace [3H]mazindol binding from rat striatal membranes	B	6.24	pIC50	580	nM	IC50	J Med Chem (1992) 35: 4764-4766 [PMID:1469704]
ChEMBL	Inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat striatal synaptic membranes	B	6.29	pIC50	510.6	nM	IC50	Bioorg Med Chem Lett (2001) 11: 3077-3080 [PMID:11714614]
ChEMBL	Inhibition of dopamine DA reuptake	B	6.32	pIC50	478	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Inhibitory activity determined for [3H]DA (Dopamine transporter) uptake by striated synaptosomes	B	6.34	pIC50	459	nM	IC50	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Tested for its ability to inhibit high affinity uptake of [3H]dopamine into rat caudate-putamen tissue	B	6.39	pIC50	405	nM	IC50	J Med Chem (1994) 37: 3875-3877 [PMID:7966147]
ChEMBL	Inhibition of dopamine uptake into rat striatal tissue, using [3H]- dopamine as the radioligand.	B	6.39	pIC50	404	nM	IC50	J Med Chem (1999) 42: 882-895 [PMID:10072685]
ChEMBL	Inhibition of [3H]DA binding to DAT in rat striatal synaptosomes.	B	6.39	pIC50	404	nM	IC50	J Med Chem (2003) 46: 1456-1464 [PMID:12672245]
ChEMBL	Inhibitory potency against [3H]DA uptake using [3H]WIN-35428 (WIN-) binding assay	B	6.39	pIC50	404	nM	IC50	J Med Chem (1999) 42: 4836-4843 [PMID:10579846]
ChEMBL	Inhibitory activity against [3H]dopamine uptake in rat striatal tissue	F	6.39	pIC50	404	nM	IC50	J Med Chem (1996) 39: 1201-1209 [PMID:8632426]
ChEMBL	Inhibitory activity on dopamine transporters of rat striated membranes using [3H]- mazindol.	B	6.4	pIC50	400	nM	IC50	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Inhibition of [3H]dopamine uptake into rat striatal synaptosomes	F	6.45	pIC50	353.1	nM	IC50	J Med Chem (2005) 48: 3337-3343 [PMID:15857139]
ChEMBL	Compound was tested for binding against Dopamine transporter using radioligand as [3H]-RTI 55	B	6.47	pIC50	341	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue	B	6.47	pIC50	338	nM	IC50	J Med Chem (2002) 45: 1203-1210 [PMID:11881989]
ChEMBL	Compound was evaluated for its ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue	B	6.47	pIC50	338	nM	IC50	J Med Chem (1997) 40: 4406-4414 [PMID:9435910]
ChEMBL	Inhibition of rat DAT-mediated [3H]dopamine uptake in CHO cells	B	6.52	pIC50	300	nM	IC50	J Med Chem (2006) 49: 4048-4051 [PMID:16821765]
ChEMBL	Functional cocaine antagonism was evaluated by inhibition of [3H]dopamine reuptake	F	6.53	pIC50	297	nM	IC50	Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356]
ChEMBL	Tested for inhibition of radioligand [3H]dopamine (DA) uptake in rat synaptosomes	B	6.53	pIC50	296	nM	IC50	J Med Chem (1993) 36: 4075-4081 [PMID:8258830]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine transporter of rat striatum	B	6.58	pIC50	266	nM	IC50	J Med Chem (2004) 47: 5101-5113 [PMID:15456254]
ChEMBL	Binding affinity was evaluated by measuring the inhibition of [3H]WIN-35428 binding to Dopamine transporter in rat brain tissue	B	6.58	pIC50	266	nM	IC50	Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726]
ChEMBL	In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement.	B	6.58	pIC50	266	nM	IC50	J Med Chem (2001) 44: 937-948 [PMID:11300876]
ChEMBL	Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement.	B	6.58	pIC50	266	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum	B	6.58	pIC50	266	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	6.58	pIC50	266	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum.	B	6.58	pIC50	266	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Inhibition of dopamine Transporter Affinity against rat whole brain using [3H]WIN-35428 as radioligand	B	6.6	pIC50	249	nM	IC50	J Med Chem (1998) 41: 2380-2389 [PMID:9632371]
ChEMBL	Compound was tested for inhibitory activity to displace [3H]WIN-35428 at dopamine transporter in Rat Striatal Membranes.	B	6.6	pIC50	249	nM	IC50	J Med Chem (1997) 40: 2474-2481 [PMID:9258354]
ChEMBL	Inhibition of high-affinity uptake of [3H]dopamine at dopamine transporter into rat striatal nerve endings (synaptosomes)	B	6.62	pIC50	239	nM	IC50	J Med Chem (1998) 41: 1962-1969 [PMID:9599245]
ChEMBL	In vitro potency for inhibiting [3H]- dopamine uptake was determined	F	6.63	pIC50	236	nM	IC50	J Med Chem (2003) 46: 2908-2916 [PMID:12825932]
ChEMBL	Inhibition of [3H]dopamine uptake at DAT in Sprague-Dawley rat brain	B	6.63	pIC50	236	nM	IC50	J Med Chem (2006) 49: 6391-6399 [PMID:17034144]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat DAT expressed in D8 cells	B	6.65	pIC50	226	nM	IC50	J Med Chem (2006) 49: 4048-4051 [PMID:16821765]
ChEMBL	Compound was tested for binding affinity to dopamine reuptake sites in the tissue homogenates prepared from primate rat striatum using [3H]CFT as radioligand	B	6.66	pIC50	221	nM	IC50	J Med Chem (1991) 34: 3144-3146 [PMID:1920365]
ChEMBL	Inhibition [3H]DA uptake in rat striatal synaptosomes.	F	6.68	pIC50	209	nM	IC50	J Med Chem (1998) 41: 864-876 [PMID:9526561]
ChEMBL	Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand	B	6.69	pIC50	205	nM	IC50	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Binding affinity for compound at site labeled by [3H]BTCP (1-[1-(2-benxo[b]thienyl)cyclohexyl]piperidine) in rat forebrain.	B	6.73	pIC50	187	nM	IC50	J Med Chem (1993) 36: 1188-1193 [PMID:8098066]
ChEMBL	Tested for radioligand [3H]BTCP displacement from dopamine transporter in rat forebrain	B	6.75	pIC50	179	nM	IC50	J Med Chem (1993) 36: 4075-4081 [PMID:8258830]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal tissue	B	6.76	pIC50	173	nM	IC50	J Med Chem (1996) 39: 1201-1209 [PMID:8632426]
ChEMBL	Inhibitory binding activity against rat striatal tissue using [3H]WIN-35248 as the radioligand.	B	6.8	pIC50	160	nM	IC50	J Med Chem (1999) 42: 882-895 [PMID:10072685]
ChEMBL	Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay.	B	6.8	pIC50	160	nM	IC50	J Med Chem (1999) 42: 4836-4843 [PMID:10579846]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the cocaine binding site on the dopamine transporter (DAT) in synaptosomal membrane preparations from rat striatal tissue.	B	6.8	pIC50	160	nM	IC50	J Med Chem (2003) 46: 1456-1464 [PMID:12672245]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the dopamine transporter.	B	6.82	pIC50	150	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Displacement of [3H]WIN-35428 from Dopamine transporter of rat caudate putamen	B	6.82	pIC50	150	nM	IC50	J Med Chem (2005) 48: 3337-3343 [PMID:15857139]
ChEMBL	Inhibition of [3H]cocaine binding to the dopamine transporter.	B	6.86	pIC50	139	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Binding affinity of compound at site labeled by [3H]-cocaine in rat forebrain.	B	6.97	pIC50	107	nM	IC50	J Med Chem (1993) 36: 1188-1193 [PMID:8098066]
ChEMBL	Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane	B	6.98	pIC50	104	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4915-4918 [PMID:16165350]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine transporter in rat striatal membranes.	B	6.99	pIC50	102	nM	IC50	J Med Chem (1993) 36: 3572-3579 [PMID:8246225]
ChEMBL	Ability to displace [3H]WIN-35428 binding to dopamine transporter from rat striatal membranes	B	6.99	pIC50	102	nM	IC50	J Med Chem (1998) 41: 1962-1969 [PMID:9599245]
ChEMBL	Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester binding to Dopamine transporter in rat striatal membranes.	B	6.99	pIC50	102	nM	IC50	J Med Chem (1992) 35: 135-140 [PMID:1732520]
ChEMBL	Inhibition of [3H]3-beta-(p-fluorophenyl)tropane-2beta-carboxylic acid methyl ester [3H]7a binding to Dopamine transporter of rat striatal membranes	B	6.99	pIC50	102	nM	IC50	J Med Chem (1992) 35: 141-144 [PMID:1732521]
ChEMBL	Inhibition of [3H]WIN-35248 binding to the dopamine transporter in rat striatal membranes.	B	6.99	pIC50	102	nM	IC50	J Med Chem (1992) 35: 1813-1817 [PMID:1588560]
ChEMBL	Inhibition of [3H]WIN-35428l binding to Dopamine transporter	B	6.99	pIC50	102	nM	IC50	J Med Chem (1992) 35: 2497-2500 [PMID:1619622]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter	B	6.99	pIC50	102	nM	IC50	J Med Chem (1991) 34: 883-886 [PMID:2002468]
ChEMBL	Inhibition of [3H]cocaine binding to Cocaine receptor in rat striatal membranes	B	7	pIC50	101	nM	IC50	J Med Chem (1998) 41: 864-876 [PMID:9526561]
ChEMBL	Displacement of 0.5 nM [3H]WIN-35248 from Dopamine transporter	B	7.05	pIC50	89.1	nM	IC50	Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197]
ChEMBL	Inhibition of [3H]WIN-35428 binding to Dopamine transporter	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (1996) 39: 4139-4141 [PMID:8863789]
ChEMBL	In vitro inhibitory activity against radioligand [3H]-WN 35,428 binding to dopamine transporter (DAT) in rat striatal tissue	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (1997) 40: 3861-3864 [PMID:9397165]
ChEMBL	Inhibitory concentration required to inhibit dopamine transporter DAT was determined by using [3H]WIN-35428 radioligand	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2004) 47: 296-302 [PMID:14711303]
ChEMBL	Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [3H]WIN-35428 binding to dopamine (DA) transporter	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (1994) 37: 1220-1223 [PMID:8164265]
ChEMBL	Inhibition of [3H]WIN-35428 binding to rat striatal dopamine transporter	B	7.05	pIC50	89.1	nM	IC50	J Med Chem (2005) 48: 3852-3857 [PMID:15916437]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat striata.	B	7.05	pIC50	89	nM	IC50	J Med Chem (1996) 39: 4027-4035 [PMID:8831768]
ChEMBL	Inhibition of [3H]WIN-35428 binding at dopamine transporter was determined	B	7.05	pIC50	89	nM	IC50	J Med Chem (2003) 46: 1775-1794 [PMID:12723940]
ChEMBL	Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand	B	7.05	pIC50	89	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL	Ability to inhibit binding of [3H]WIN-35428 to dopamine transporter in rat caudate putamen	B	7.05	pIC50	89	nM	IC50	Bioorg Med Chem Lett (2001) 11: 823-827 [PMID:11277529]
ChEMBL	Binding affinity at the Dopamine transporter in rat striata by inhibition of 0.5 nM [3H]WIN-35428 binding	B	7.05	pIC50	89	nM	IC50	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Inhibitory activity against Dopamine transporter using 0.5 nM [3H]WIN-35428 as radioligand	B	7.05	pIC50	89	nM	IC50	J Med Chem (1997) 40: 1247-1251 [PMID:9111298]
ChEMBL	Inhibitory activity against radioligand [3H]WIN-35428 binding at the dopamine transporter	B	7.05	pIC50	89	nM	IC50	Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496]
ChEMBL	Binding affinity towards dopamine transporter was determined using DA[3H]WIN-35428 as radioligand	B	7.05	pIC50	89	nM	IC50	J Med Chem (1995) 38: 3451-3453 [PMID:7658431]
ChEMBL	Tested for radioligand [3H]cocaine displacement from dopamine transporter in rat forebrain	B	7.09	pIC50	82	nM	IC50	J Med Chem (1993) 36: 4075-4081 [PMID:8258830]
GtoPdb	-	-	7.1	pIC50	89.1	nM	IC50	J Med Chem (2004) 47: 6401-9 [PMID:15566309]
ChEMBL	Tested for inhibition of [3H]cocaine binding to rat striatal P2 membranes	B	7.15	pIC50	70	nM	IC50	J Med Chem (1994) 37: 2249-2252 [PMID:8035432]
ChEMBL	Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys	B	7.17	pIC50	67.8	nM	IC50	J Med Chem (1991) 34: 1728-1731 [PMID:2033595]
ChEMBL	Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.	B	7.18	pIC50	66	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL	Tested for affinity by radioligand [3H]-TCP displacement from phencyclidine binding site (PCP) in rat homogenates	B	5	pKi	>10000	nM	Ki	J Med Chem (1993) 36: 4075-4081 [PMID:8258830]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human Potassium channel HERG expressed in mammalian cells	B	5.14	pIC50	7244.36	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL	Inhibitory concentration against potassium channel HERG	B	5.14	pIC50	7244.36	nM	IC50	Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL	Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique	B	5.14	pIC50	7244.36	nM	IC50	Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL	Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel)	F	5.24	pIC50	5754.4	nM	IC50	Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL	Inhibition of human ERG in MCF7 cells	B	5.24	pIC50	5754.4	nM	IC50	Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL	K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1	F	8.36	pIC50	4.4	nM	IC50	J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL	Binding affinity at muscarinic M1 receptor in rat brain by [3H]pirenzepine displacement.	B	4.21	pKi	61400	nM	Ki	J Med Chem (2004) 47: 3388-3398 [PMID:15189035]
ChEMBL	Displacement of [3H]pirenzepine from M1 receptor in Sprague-Dawley rat brain	B	4.21	pKi	61400	nM	Ki	J Med Chem (2006) 49: 6391-6399 [PMID:17034144]
ChEMBL	Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane	B	4.21	pKi	61397	nM	Ki	Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	Inhibition of [3H]mazindol binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	4.97	pKi	10700	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Binding affinity against norepinephrine cloned human transporter using 40-80 pM [125I]RTI	B	5.57	pKi	2700	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Inhibition of [125I]RTI-55 binding to recombinant human NET expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	5.62	pKi	2410	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting	B	5.62	pKi	2377	nM	Ki	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Displacement of [125I]RTI-55 from human NET expressed in HEK293 cell membranes	B	5.63	pKi	2357	nM	Ki	J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
ChEMBL	Displacement of [125I]RTI-55 from human NET expressed in HEK293 cells	B	5.67	pKi	2150	nM	Ki	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Displacement of [3H]nisoxetine from NET	B	5.7	pKi	1990	nM	Ki	J Med Chem (2005) 48: 7437-7444 [PMID:16279803]
ChEMBL	Displacement of [3H]nisoxetine from human NET	B	5.7	pKi	1990	nM	Ki	J Med Chem (2006) 49: 4589-4594 [PMID:16854064]
ChEMBL	Displacement of [3H]nisoxetine from NET	B	5.7	pKi	1990	nM	Ki	J Med Chem (2004) 47: 6401-6409 [PMID:15566309]
ChEMBL	Displacement of [3H]nisoxetine from norepinephrine transporter	B	5.7	pKi	1990	nM	Ki	Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164]
ChEMBL	Displacement of [3H]nisoxetine from NET	B	5.7	pKi	1990	nM	Ki	Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837]
ChEMBL	Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells	B	5.71	pKi	1940	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Binding affinity at the norepinephrine transporter was measured using [125I]RTI-55 as a radioligand	B	5.75	pKi	1770	nM	Ki	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [125I]RTI-55 binding to norepinephrine transporter (NET) expressed in HEK cells	B	5.75	pKi	1770	nM	Ki	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hNET cells expressing human norepinephrine transporter	B	5.76	pKi	1740	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
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	5.9	pKi	1257	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [125I]RTI55 from human NET expressed in HEK cells	B	5.95	pKi	1116	nM	Ki	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant NET expressed in HEK293 cells by scintillation counting	B	5.95	pKi	1115	nM	Ki	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	Displacement of [125I]RTI55 from human recombinant NET expressed in HEK293 cells	B	5.95	pKi	1115	nM	Ki	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Displacement of [125I]RTI55 from human NET expressed in COS1 cell membrane	B	6.05	pKi	887	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
ChEMBL	Displacement of [125I]RTI55 from cloned human NET expressed in HEK293 cells	B	6.08	pKi	830	nM	Ki	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Compound was tested for inhibition of [125I]-RTI-55 binding to norepinephrine transporter HEK cells	B	6.08	pKi	830	nM	Ki	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Displacement of [125I]RT155 binding in HEK cells expressing human NET	B	6.19	pKi	645	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	Displacement of [125I]RTI-55 from human NET expressing HEK293 cells	B	6.3	pKi	500	nM	Ki	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Compound was evaluated for inhibition of [3H]NE uptake in HEK-hNET cells expressing Human norepinephrine transporter	B	6.58	pKi	264	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Inhibition of reuptake of [3H]-NE (20 nM) by norepinephrine transporter	B	6.72	pKi	190	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Inhibition of [3H]DA uptake in human NET expressed in COS1 cell membrane	F	6.74	pKi	182	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
ChEMBL	Inhibition of [3H]-NE uptake evaluated at the monoamine transporter (NET)	B	6.97	pKi	108	nM	Ki	Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962]
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	5.2	pIC50	6309.57	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [3H]nisoxetine from NET	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2005) 48: 7437-7444 [PMID:16279803]
ChEMBL	Displacement of [3H]nisoxetine from NET	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2004) 47: 6401-6409 [PMID:15566309]
ChEMBL	Displacement of [3H]nisoxetine from human NET	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2006) 49: 4589-4594 [PMID:16854064]
ChEMBL	Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK293 cells	B	5.52	pIC50	2990	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells	B	5.72	pIC50	1900	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
ChEMBL	Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK cells	B	5.89	pIC50	1281	nM	IC50	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Inhibition of rat NET-mediated norepinephrine uptake in CHO cells	B	6.05	pIC50	900	nM	IC50	J Med Chem (2006) 49: 4048-4051 [PMID:16821765]
ChEMBL	Displacement of [3H]norepinephrine from human recombinant NET expressed in HEK293 cells by scintillation counting	B	6.08	pIC50	835	nM	IC50	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	Inhibition of [3H]NE from human recombinant NET expressed in HEK293 cells	B	6.08	pIC50	835	nM	IC50	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Inhibition of [3H]norepinephrine uptake in HEK293 cells expressing human norepinephrine transporter	F	6.34	pIC50	462	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Compound was tested for inhibition of [3H]NE binding to norepinephrine transporter HEK cells	B	6.41	pIC50	385	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells	B	6.41	pIC50	385	nM	IC50	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Inhibition of [3H] norepinephrine uptake into human NET expressed in HEK293 cells	F	6.42	pIC50	378	nM	IC50	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Inhibition of NE uptake in HEK cells expressing human noradrenaline transporter (hNET)	F	6.63	pIC50	233	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [3H]NE reuptake at human NET expressed in HEK cells	B	6.63	pIC50	232	nM	IC50	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells	B	6.64	pIC50	230	nM	IC50	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [3H]- NE uptake in HEK cells expressing norepinephrine transporter	F	6.64	pIC50	230	nM	IC50	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis	B	6.66	pIC50	221	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [3H]NE uptake into human NET expressing HEK293 cells	B	6.68	pIC50	210	nM	IC50	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET	B	6.72	pIC50	192	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	The compound was tested for inhibition of [3H]norepinephrine uptake in HEK cells by expressing cDNA for human norepinephrine transporter	B	6.73	pIC50	186	nM	IC50	Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458]
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	4.52	pKi	>30000	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex	B	5.48	pKi	3320	nM	Ki	Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL	Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane	B	5.48	pKi	3302	nM	Ki	Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693]
ChEMBL	Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain	B	5.48	pKi	3300	nM	Ki	J Med Chem (2006) 49: 6391-6399 [PMID:17034144]
ChEMBL	Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat brain	B	5.48	pKi	3300	nM	Ki	J Med Chem (2004) 47: 3388-3398 [PMID:15189035]
ChEMBL	The compound was tested for binding affinity nisoxatine ligand	B	5.48	pKi	3300	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined	B	5.7	pKi	2000	nM	Ki	J Med Chem (2003) 46: 1775-1794 [PMID:12723940]
ChEMBL	Binding affinity towards norepinephrine transporter was determined using [3H]nisoxetine radioligand.	B	5.7	pKi	1990	nM	Ki	J Med Chem (2004) 47: 296-302 [PMID:14711303]
ChEMBL	Inhibition of 0.5 nM [3H]nisoxetine binding to Norepinephrine transporter	B	5.72	pKi	1900	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197]
ChEMBL	Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat cerebral cortex	B	5.72	pKi	1900	nM	Ki	J Med Chem (2005) 48: 3852-3857 [PMID:15916437]
ChEMBL	Inhibition of [3H]NE uptake at Norepinephrine transporter in rat parietal/occipital cortex was determined	B	6.72	pKi	190	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356]
ChEMBL	Inhibition of [3H]NE binding to norepinephrine transporter of rat brain synaptosomes	B	6.73	pKi	186	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724]
ChEMBL	Inhibition of [3H]NE uptake by rat frontal cortex Norepinephrine transporter	B	6.79	pKi	160.55	nM	Ki	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Displacement of [3H]NE from Norepinephrine transporter of rat brain	B	6.97	pKi	108	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143]
ChEMBL	Inhibition of [3H]NE Uptake in rat parietal/occipital cortex	B	6.97	pKi	108	nM	Ki	J Med Chem (2000) 43: 351-360 [PMID:10669562]
ChEMBL	Ability to inhibit [3H]NE reuptake at norepinephrine transporter from rat brain	B	6.97	pKi	108	nM	Ki	J Med Chem (2003) 46: 1997-2007 [PMID:12723962]
ChEMBL	Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes	B	6.97	pKi	108	nM	Ki	J Med Chem (2000) 43: 1215-1222 [PMID:10737754]
ChEMBL	Ability to inhibit high affinity uptake of norepinephrine transporter into the nerve endings of rat synaptosomes using [3H]NE as a radioligand	B	6.97	pKi	108	nM	Ki	J Med Chem (2001) 44: 1615-1622 [PMID:11334571]
ChEMBL	Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region	B	6.97	pKi	108	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL	Inhibition of reuptake of [3H]-NE at Norepinephrine transporter	B	6.97	pKi	108	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Compound was tested for its ability to inhibit high-affinity uptake of [3H]NE into parietal and occipital cortex in rat	B	6.97	pKi	108	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328]
ChEMBL	Inhibition of high affinity uptake of [3H]NE by norepinephrine transporter in nerve endings obtained from rat brain.	B	6.97	pKi	108	nM	Ki	J Med Chem (2002) 45: 3161-3170 [PMID:12109901]
ChEMBL	Ability to inhibit high affinity uptake of [3H]NE at Norepinephrine transporter (NET) using rat brain parietal/occipital cortex	B	6.97	pKi	108	nM	Ki	J Med Chem (2004) 47: 3009-3018 [PMID:15163183]
ChEMBL	Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex	B	6.97	pKi	108	nM	Ki	Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701]
ChEMBL	Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions	B	6.97	pKi	108	nM	Ki	J Med Chem (2002) 45: 1930-1941 [PMID:11960503]
ChEMBL	Inhibition of high affinity uptake by the norepinephrine transporter from rat synaptosomal nerve endings by using [3H]NE as radioligand	B	6.97	pKi	108	nM	Ki	J Med Chem (2004) 47: 5821-5824 [PMID:15537337]
ChEMBL	Inhibition of [3H]mazindol binding to Norepinephrine transporter	B	5.42	pIC50	3825	nM	IC50	J Med Chem (1992) 35: 2497-2500 [PMID:1619622]
ChEMBL	Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum	B	5.45	pIC50	3530	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762]
ChEMBL	Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Inhibition of [3H]nisoxetine binding to norepinephrine transporter of rat cerebral cortex	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2004) 47: 5101-5113 [PMID:15456254]
ChEMBL	Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2001) 44: 937-948 [PMID:11300876]
ChEMBL	Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement.	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex.	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Binding affinity was evaluated by measuring inhibiting the binding of [3H]nisoxetine to Norepinephrine transporter in rat brain tissue	B	5.45	pIC50	3520	nM	IC50	Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726]
ChEMBL	Inhibition of [3H]nisoxetine binding to rat cerebral cortex norepinephrine transporter	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2005) 48: 3852-3857 [PMID:15916437]
ChEMBL	Inhibition of norepinephrine transporter (NET) determined using [3H]nisoxetine radioligand.	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2004) 47: 296-302 [PMID:14711303]
ChEMBL	In vitro inhibitory activity against radioligand [3H]-nisoxatine binding to norepinephrine transporter (NET) in rat cortical tissue	B	5.48	pIC50	3300	nM	IC50	J Med Chem (1997) 40: 3861-3864 [PMID:9397165]
ChEMBL	Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined	B	5.48	pIC50	3300	nM	IC50	J Med Chem (2003) 46: 1775-1794 [PMID:12723940]
ChEMBL	Norepinephrine transporter activity was determined by the ability of compound to inhibit the neurotransmitter norepinephrine-NE reuptake system using [3H]norepinephrine as radioligand	B	5.48	pIC50	3300	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL	Inhibition of 0.5 nM [3H]nisoxetine binding toNorepinephrine transporter	B	5.48	pIC50	3300	nM	IC50	Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197]
ChEMBL	Inhibitory activity against radioligand [3H]nisoxetine binding at the norepinephrine transporter	B	5.48	pIC50	3300	nM	IC50	Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496]
ChEMBL	Inhibitory activity against Norepinephrine transporter using 0.5 nM [3H]-radioligand	B	5.48	pIC50	3300	nM	IC50	J Med Chem (1997) 40: 1247-1251 [PMID:9111298]
ChEMBL	Selectivity for the norepinephrine transporter using [3H]nisoxetine binding assay	B	5.48	pIC50	3300	nM	IC50	J Med Chem (1999) 42: 4836-4843 [PMID:10579846]
ChEMBL	Binding affinity at the Norepinephrine transporter in rat frontal cortex by inhibition of 0.5 nM [3H]nisoxetine binding	B	5.48	pIC50	3298	nM	IC50	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter	B	5.48	pIC50	3298	nM	IC50	J Med Chem (1994) 37: 1220-1223 [PMID:8164265]
ChEMBL	Binding affinity towards Norepinephrine transporter was determined using NE[3H]Nisoxetine as radioligand	B	5.48	pIC50	3298	nM	IC50	J Med Chem (1995) 38: 3451-3453 [PMID:7658431]
ChEMBL	Binding potency for Norepinephrine transporter using [3H]NE	B	5.48	pIC50	3298	nM	IC50	J Med Chem (1996) 39: 4139-4141 [PMID:8863789]
ChEMBL	Inhibition of [3H]nisoxetine binding to the norepinephrine transporter in rat midbrain.	B	5.48	pIC50	3298	nM	IC50	J Med Chem (1996) 39: 4027-4035 [PMID:8831768]
ChEMBL	Inhibition of norepinephrine Transporter Affinity against rat whole brain using [3H]nisoxetine radioligand	B	5.6	pIC50	2500	nM	IC50	J Med Chem (1998) 41: 2380-2389 [PMID:9632371]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Displacement of [125I]RTI55 from human SERT expressed in COS1 cell membrane	B	6.02	pKi	965	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
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	6.09	pKi	818	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of [125I]RTI-55 binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	6.18	pKi	657	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cell membranes	B	6.2	pKi	632	nM	Ki	J Med Chem (2018) 61: 9121-9131 [PMID:30240563]
ChEMBL	Displacement of [125I]RTI55 from cloned human SERT expressed in HEK293 cells	B	6.22	pKi	601	nM	Ki	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Compound was tested for inhibition of [125I]RTI-55 binding to Serotonin transporter in HEK cells	B	6.22	pKi	601	nM	Ki	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells	B	6.28	pKi	525	nM	Ki	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Inhibition of [3H]SER uptake in human SERT expressed in COS1 cell membrane	F	6.28	pKi	524	nM	Ki	Bioorg Med Chem (2007) 15: 4159-4174 [PMID:17446076]
ChEMBL	Binding affinity against cloned serotonin human transporter using 40-80 PM [125I]RTI	B	6.3	pKi	500	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Binding affinity for serotonin transporter using [125I]RTI-55	B	6.41	pKi	390	nM	Ki	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [125I]RTI-55 binding to serotonin transporter (SERT) expressed in HEK cells	B	6.41	pKi	387	nM	Ki	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Displacement of [125I]RTI-55 from human SERT expressed in HEK293 cells	B	6.45	pKi	358	nM	Ki	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hSERT cells expressing human serotonin transporter	B	6.46	pKi	343	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Displacement of [125I]RTI-55 from human SERT expressing HEK293 cells	B	6.47	pKi	340	nM	Ki	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Displacement of [125I]- RTI-55 from Serotonin transporter expressed in HEK cells	B	6.48	pKi	328	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of reuptake of [3H]5-HT (20 nM) by serotonin transporter	B	6.51	pKi	310	nM	Ki	J Med Chem (2000) 43: 4981-4992 [PMID:11150168]
ChEMBL	Compound was evaluated for inhibition of [3H]5-HT uptake in HEK-hSERT cells expressing Human serotonin transporter	B	6.52	pKi	301	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Displacement of [125I]RT155 binding in HEK cells expressing human SERT	B	6.53	pKi	297	nM	Ki	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	Displacement of [125I]RTI55 from human recombinant SERT expressed in HEK293 cells	B	6.56	pKi	276	nM	Ki	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Displacement of [125I]RTI-55 from human recombinant SERT expressed in HEK293 cells by scintillation counting	B	6.56	pKi	276	nM	Ki	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	Displacement of [125I]RTI55 from human SERT expressed in HEK cells	B	6.56	pKi	276	nM	Ki	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Inhibition of [3H]mazindol binding to recombinant human SERT expressed in HEK293 cell membranes preincubated for 10 mins followed by radioligand addition measured after 90 mins by micro beta scintillation counting analysis	B	6.64	pKi	229	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [3H]-5-HT uptake evaluated at the Serotonin transporter	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2003) 13: 513-517 [PMID:12565962]
ChEMBL	Binding affinity at SERT	B	6.89	pKi	129	nM	Ki	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Displacement of [3H]paroxetine from 5-HTT	B	7.02	pKi	95	nM	Ki	Bioorg Med Chem (2009) 17: 5126-5132 [PMID:19523837]
ChEMBL	Displacement of [3H]paroxetine from serotonin transporter	B	7.02	pKi	95	nM	Ki	Bioorg Med Chem (2008) 16: 5529-5535 [PMID:18434164]
ChEMBL	Displacement of [3H]paroxetine from 5HTT	B	7.35	pKi	45	nM	Ki	J Med Chem (2005) 48: 7437-7444 [PMID:16279803]
ChEMBL	Displacement of [3H]paroxetine from 5HTT	B	7.35	pKi	45	nM	Ki	J Med Chem (2004) 47: 6401-6409 [PMID:15566309]
ChEMBL	Displacement of [3H]paroxetine from human 5HTT	B	7.35	pKi	45	nM	Ki	J Med Chem (2006) 49: 4589-4594 [PMID:16854064]
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	5.62	pIC50	2398.83	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [3H]paroxetine from 5HTT	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2004) 47: 6401-6409 [PMID:15566309]
ChEMBL	Displacement of [3H]paroxetine from 5HTT	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2005) 48: 7437-7444 [PMID:16279803]
ChEMBL	Displacement of [3H]paroxetine from human 5HTT	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2006) 49: 4589-4594 [PMID:16854064]
ChEMBL	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK cells	B	6.19	pIC50	642	nM	IC50	Bioorg Med Chem (2009) 17: 2047-2068 [PMID:19201198]
ChEMBL	Displacement of [3H]citalopram from human SERT expressed in HEK293 cell membrane	B	6.27	pIC50	540	nM	IC50	Bioorg Med Chem Lett (2011) 21: 48-51 [PMID:21146984]
ChEMBL	Inhibition of [3H] serotonin uptake into human SERT expressed in HEK293 cells	F	6.31	pIC50	494	nM	IC50	J Med Chem (2006) 49: 1420-1432 [PMID:16480278]
ChEMBL	Displacement of [125I]RTI-55 from human Serotonin transporter expressed in HEK293 cells	B	6.36	pIC50	433	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Inhibition of [3H]5HT from human recombinant SERT expressed in HEK293 cells	B	6.38	pIC50	416	nM	IC50	Bioorg Med Chem (2009) 17: 337-343 [PMID:19014888]
ChEMBL	Displacement of [3H]serotonin from human recombinant SERT expressed in HEK293 cells by scintillation counting	B	6.38	pIC50	416	nM	IC50	J Med Chem (2009) 52: 1530-1539 [PMID:19256502]
ChEMBL	The compound was tested for inhibition of [3H]-5-hydroxy tryptamine uptake in HEK cells by expressing cDNA for human tryptamine transporter	B	6.38	pIC50	413	nM	IC50	Bioorg Med Chem Lett (2000) 10: 297-300 [PMID:10698458]
ChEMBL	Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter	B	6.47	pIC50	340	nM	IC50	J Med Chem (2000) 43: 205-213 [PMID:10649976]
ChEMBL	Inhibition of [3H]5HT reuptake at human SERT expressed in HEK293 cells	B	6.47	pIC50	338	nM	IC50	Bioorg Med Chem (2009) 17: 6890-6897 [PMID:19740668]
ChEMBL	Inhibition of 5-HT uptake in HEK cells expressing human serotonin transporter (hSERT)	F	6.47	pIC50	338	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [3H]- 5-HT uptake in HEK cells expressing serotonin transporter	F	6.47	pIC50	336	nM	IC50	J Med Chem (1999) 42: 3647-3656 [PMID:10479296]
ChEMBL	Inhibition of [3H]5-HT uptake in HEK cells expressing human SERT	B	6.49	pIC50	325	nM	IC50	Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523]
ChEMBL	Compound was tested for inhibition of [3H]5-HT binding to Serotonin transporter in HEK cells	B	6.5	pIC50	318	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2151-2154 [PMID:12798324]
ChEMBL	Inhibition of [3H]serotonin reuptake at human SERT expressed in HEK293 cells	B	6.5	pIC50	318	nM	IC50	J Med Chem (2009) 52: 6768-6781 [PMID:19821577]
ChEMBL	Inhibition of [3H]5HT uptake in SERT	B	6.52	pIC50	304	nM	IC50	J Med Chem (2008) 51: 2795-2806 [PMID:18393401]
ChEMBL	Inhibition of [3H]5-HT uptake in HEK293 cells expressing human serotonin transporter	F	6.54	pIC50	289	nM	IC50	J Med Chem (2005) 48: 2876-2881 [PMID:15828826]
ChEMBL	Inhibition of recombinant human SERT expressed in HEK293 cell membranes assessed as reduction in [3H]5-HT uptake incubated for 22 mins by micro beta scintillation counting analysis	B	6.56	pIC50	277	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [3H]citalopram binding to serotonin transporter (SERT) of cynomolgus monkey caudate-putamen	B	6.57	pIC50	270	nM	IC50	Bioorg Med Chem Lett (1999) 9: 857-862 [PMID:10206550]
ChEMBL	Ability to inhibit [3H]citalopram binding to serotonin transporter in cynomolgus monkey striatum	B	6.57	pIC50	270	nM	IC50	J Med Chem (1993) 36: 855-862 [PMID:8464040]
ChEMBL	Inhibition of [3H]5-HT uptake into human SERT expressing HEK293 cells	B	6.6	pIC50	250	nM	IC50	J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL	Inhibition of [3H]5HT uptake at human SERT expressed in HEK293 cells	B	6.74	pIC50	180	nM	IC50	Antimicrob Agents Chemother (2007) 51: 4133-4140 [PMID:17846138]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement.	B	5	pKi	>10000	nM	Ki	J Med Chem (1996) 39: 543-548 [PMID:8558525]
ChEMBL	Displacement of [3H]paroxetine from serotonin transporter of rat cerebral cortex	B	5.98	pKi	1050	nM	Ki	Bioorg Med Chem Lett (2005) 15: 1131-1133 [PMID:15686927]
ChEMBL	Inhibition of [3H]-5-HT binding to serotonin transporter of rat brain synaptosomes	B	6.38	pKi	413	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1681-1686 [PMID:10937724]
ChEMBL	Displacement of [3H]-citalopram from serotonin transporter of rat brain membrane	B	6.53	pKi	293	nM	Ki	Bioorg Med Chem Lett (2004) 14: 3295-3298 [PMID:15149693]
ChEMBL	Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain membranes	B	6.54	pKi	286	nM	Ki	ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069]
ChEMBL	Displacement of [3H]citalopram from SERT in rat brain	B	6.54	pKi	286	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846]
ChEMBL	Binding affinity at serotonin transporter in rat brain by [3H]-citalopram displacement.	B	6.54	pKi	286	nM	Ki	J Med Chem (2004) 47: 3388-3398 [PMID:15189035]
ChEMBL	Displacement of [3H]citalopram from SERT in Sprague-Dawley rat brain	B	6.54	pKi	286	nM	Ki	J Med Chem (2006) 49: 6391-6399 [PMID:17034144]
ChEMBL	Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand	B	6.76	pKi	172	nM	Ki	J Med Chem (1999) 42: 4446-4455 [PMID:10543888]
ChEMBL	Inhibition of [3H]5-HT uptake at striatal nerve endings by serotonin transporter	B	6.8	pKi	160	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3325-3328 [PMID:10612593]
ChEMBL	Inhibition of [3H]5-HT uptake at Serotonin transporter in rat mid brain	B	6.8	pKi	160	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1113-1118 [PMID:11354356]
ChEMBL	Compound was tested for its ability to inhibit high affinity uptake of [3H]5-HT into mid brain nerve endings (synaptosomes) in rat	B	6.8	pKi	160	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328]
ChEMBL	Inhibition of high affinity uptake of [3H]5-HT by serotonin transporter in nerve endings obtained from rat brain.	B	6.81	pKi	155	nM	Ki	J Med Chem (2002) 45: 3161-3170 [PMID:12109901]
ChEMBL	Inhibition of [3H]5-HT Uptake in rat mid brain.	B	6.81	pKi	155	nM	Ki	J Med Chem (2000) 43: 351-360 [PMID:10669562]
ChEMBL	Ability to inhibit [3H]5-HT reuptake at serotonin transporter from rat brain	B	6.81	pKi	155	nM	Ki	J Med Chem (2003) 46: 1997-2007 [PMID:12723962]
ChEMBL	Inhibition of [3H]5-HT uptake by Serotonin transporter of rat midbrain or parietal synaptosomes	B	6.81	pKi	155	nM	Ki	J Med Chem (2000) 43: 1215-1222 [PMID:10737754]
ChEMBL	Inhibition of high affinity serotonin uptake into rat synaptosomes using [3H]5-HT	B	6.81	pKi	155	nM	Ki	J Med Chem (2001) 44: 1615-1622 [PMID:11334571]
ChEMBL	Ability to inhibit reuptake of serotonin ([3H]5-HT) at serotonin transporter of rat midbrian	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3565-3569 [PMID:14505672]
ChEMBL	Inhibition of reuptake of [3H]5-HT at serotonin transporter	B	6.81	pKi	155	nM	Ki	J Med Chem (2000) 43: 2064-2071 [PMID:10821718]
ChEMBL	Displacement of [3H]5-HT from serotonin transporter of rat brain	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2079-2083 [PMID:11514143]
ChEMBL	Ability to inhibit high affinity uptake of [3H]-5-HT at Serotonin transporter (SERT) using rat midbrain	B	6.81	pKi	155	nM	Ki	J Med Chem (2004) 47: 3009-3018 [PMID:15163183]
ChEMBL	Inhibition of [3H]5-HT reuptake at serotonin transporter in rat mid brain	B	6.81	pKi	155	nM	Ki	Bioorg Med Chem Lett (2002) 12: 993-995 [PMID:11909701]
ChEMBL	Binding affinity for Serotonin transporter was determined by [3H]5-HT (serotonin) uptake by striated synaptosomes	B	6.81	pKi	155	nM	Ki	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Inhibition of high affinity re-uptake of [3H]5-HT (serotonin) into nerve ending synaptosomes	B	6.81	pKi	155	nM	Ki	J Med Chem (2002) 45: 1930-1941 [PMID:11960503]
ChEMBL	Inhibition of high affinity uptake by the serotonin transporter (5-HT) from rat synaptosomal nerve endings by using [3H]5-HT as radioligand	B	6.81	pKi	155	nM	Ki	J Med Chem (2004) 47: 5821-5824 [PMID:15537337]
ChEMBL	Inhibition of [125I]RTI-55 binding to Serotonin transporter of rat caudate membranes	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2225-2228 [PMID:12127543]
ChEMBL	Ratio of Ki value towards Serotonin transporter to that of dopamine transporter	B	6.95	pKi	112.11	nM	Ki	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Inhibition of [3H]paroxetine binding at serotonin transporter was determined	B	7.02	pKi	96	nM	Ki	J Med Chem (2003) 46: 1775-1794 [PMID:12723940]
ChEMBL	Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter	B	7.02	pKi	95	nM	Ki	Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197]
ChEMBL	Displacement of [3H]paroxetine from serotonin transporter (5-HT) of rat cerebral cortex	B	7.02	pKi	95	nM	Ki	J Med Chem (2005) 48: 3852-3857 [PMID:15916437]
ChEMBL	Binding affinity towards serotonin transporter 5-HTT was determined using [3H]paroxetine radioligand.	B	7.35	pKi	45	nM	Ki	J Med Chem (2004) 47: 296-302 [PMID:14711303]
ChEMBL	Inhibition of [3H]paroxetine binding to Serotonin transporter	B	5.98	pIC50	1059	nM	IC50	J Med Chem (1992) 35: 2497-2500 [PMID:1619622]
ChEMBL	Selectivity for the Serotonin transporter using [3H]paroxetine binding assay	B	5.98	pIC50	1050	nM	IC50	J Med Chem (1999) 42: 4836-4843 [PMID:10579846]
ChEMBL	Inhibitory activity against Serotonin transporter using 0.2 nM [3H]paroxetine as radioligand	B	5.98	pIC50	1050	nM	IC50	J Med Chem (1997) 40: 1247-1251 [PMID:9111298]
ChEMBL	Inhibitory concentration required to inhibit serotonin transporter 5-HTT was determined by using [3H]paroxetine radioligand	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2004) 47: 296-302 [PMID:14711303]
ChEMBL	In vitro inhibitory activity against radioligand [3H]paroxetine binding to serotonin transporter (5-HTT) in rat midbrain tissue	B	5.98	pIC50	1050	nM	IC50	J Med Chem (1997) 40: 3861-3864 [PMID:9397165]
ChEMBL	Inhibition of [3H]paroxetine binding at serotonin transporter was determined	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2003) 46: 1775-1794 [PMID:12723940]
ChEMBL	Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter	B	5.98	pIC50	1050	nM	IC50	Bioorg Med Chem Lett (2000) 10: 2445-2447 [PMID:11078197]
ChEMBL	Inhibition of [3H]paroxetine binding to rat cortex serotonin transporter	B	5.98	pIC50	1050	nM	IC50	J Med Chem (2005) 48: 3852-3857 [PMID:15916437]
ChEMBL	Inhibitory activity against radioligand [3H]paroxetine binding at the serotonin transporter	B	5.98	pIC50	1050	nM	IC50	Bioorg Med Chem Lett (1998) 8: 3689-3692 [PMID:9934496]
ChEMBL	Compound was tested for its ability to inhibit the neurotransmitter serotonin-5-HT reuptake system using [3H]5-HT as radioligand	B	5.98	pIC50	1045	nM	IC50	Bioorg Med Chem Lett (1997) 7: 2559-2564
ChEMBL	Binding affinity towards Serotonin transporter was determined using 5-HT [3H]paroxetine as radioligand	B	5.98	pIC50	1045	nM	IC50	J Med Chem (1995) 38: 3451-3453 [PMID:7658431]
ChEMBL	Binding affinity at the Serotonin transporter in rat midbrain by inhibition of 0.5 nM [3H]-paroxetine binding	B	5.98	pIC50	1045	nM	IC50	J Med Chem (1995) 38: 379-388 [PMID:7830281]
ChEMBL	Inhibition of [3H]paroxetine binding to serotonin transporter in rat frontal cortex	B	5.98	pIC50	1045	nM	IC50	J Med Chem (1996) 39: 4027-4035 [PMID:8831768]
ChEMBL	Inhibition of [3H]paroxetine binding to 5-hydroxytryptamine (5-HT) transporter	B	5.98	pIC50	1045	nM	IC50	J Med Chem (1994) 37: 1220-1223 [PMID:8164265]
ChEMBL	Binding potency for Serotonin transporter using [3H]- paroxetine	B	5.98	pIC50	1045	nM	IC50	J Med Chem (1996) 39: 4139-4141 [PMID:8863789]
ChEMBL	Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement.	B	6.13	pIC50	737	nM	IC50	J Med Chem (2003) 46: 2205-2215 [PMID:12747792]
ChEMBL	Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum	B	6.13	pIC50	737	nM	IC50	Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762]
ChEMBL	Inhibition of [3H]citalopram binding to serotonin transporter of rat cerebral cortex	B	6.13	pIC50	737	nM	IC50	J Med Chem (2004) 47: 5101-5113 [PMID:15456254]
ChEMBL	In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement.	B	6.13	pIC50	737	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	6.13	pIC50	737	nM	IC50	J Med Chem (2002) 45: 654-662 [PMID:11806716]
ChEMBL	Binding affinity was evaluated by measuring inhibiting the binding of [3H]citalopram to Serotonin transporter in rat brain tissue	B	6.13	pIC50	737	nM	IC50	Bioorg Med Chem Lett (2001) 11: 2337-2340 [PMID:11527726]
ChEMBL	Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand	B	6.13	pIC50	737	nM	IC50	J Med Chem (2003) 46: 1220-1228 [PMID:12646032]
ChEMBL	Inhibition of serotonin Transporter Affinity against rat whole brain using [3H]paroxetine as radioligand	B	6.21	pIC50	615	nM	IC50	J Med Chem (1998) 41: 2380-2389 [PMID:9632371]
ChEMBL	Inhibition of rat SERT-mediated serotonin uptake in CHO cells	B	6.4	pIC50	400	nM	IC50	J Med Chem (2006) 49: 4048-4051 [PMID:16821765]
ChEMBL	Inhibition of [3H]citalopram binding to Serotonin transporter (5-HTT) in rat cortical tissue.	B	6.41	pIC50	389	nM	IC50	J Med Chem (2003) 46: 1456-1464 [PMID:12672245]
ChEMBL	Inhibition of [3H]5-HT reuptake at rat serotonin transporter	B	6.52	pIC50	304	nM	IC50	J Med Chem (1996) 39: 4704-4716 [PMID:8941383]
ChEMBL	Compound was tested for binding affinity to Serotonin transporter sites in homogenates prepared from rat cortical membranes using [3H]paroxetine as radioligand	B	6.68	pIC50	207	nM	IC50	J Med Chem (1991) 34: 3144-3146 [PMID:1920365]
ChEMBL	Inhibitory activity against Serotonin transporter was determined for [3H]5-HT (serotonin) uptake by striated synaptosomes	B	6.77	pIC50	168	nM	IC50	J Med Chem (1998) 41: 4973-4982 [PMID:9836615]
ChEMBL	Displacement of [3H]paroxetine from Serotonin transporter of rat caudate putamen	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2005) 48: 3337-3343 [PMID:15857139]
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	5.05	pKi	8830	nM	Ki	J Med Chem (2003) 46: 2589-2598 [PMID:12801223]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain membranes	B	5.48	pKi	3300	nM	Ki	ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069]
ChEMBL	Displacement of [3H]nisoxetine from NET in rat brain	B	5.5	pKi	3192	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6865-6868 [PMID:19896846]
5-HT3AB in Human [GtoPdb: 378]
GtoPdb	-	-	4.8	pKi	-	-	-	Neuropharmacology (2001) 41: 282-4 [PMID:11489465]
5-HT3A in Human [GtoPdb: 379]
GtoPdb	-	-	5.4	pKi	-	-	-	Neuropharmacology (2001) 41: 282-4 [PMID:11489465]; Br J Pharmacol (1996) 118: 1237-45 [PMID:8818349]

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]