ChEMBL ligand: CHEMBL781 (42-548, AN-448, Magrilon, Mazanor, Mazildene, Mazindol, Mazindol civ, SAH-42548, Sanorex, Terenac, Teronac)
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!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
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!

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	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	7.13	pKi	74.2	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of [125I]- RTI -55 binding at the Dopamine transporter sites on HEK-hDAT cells	B	7.35	pKi	45	nM	Ki	J Med Chem (2002) 45: 4110-4118 [PMID:12213054]
ChEMBL	Displacement of [125I]- RTI-55 from Dopamine transporter expressed in HEK cells	B	7.35	pKi	45	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
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	7.46	pKi	34.6	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells	B	7.66	pKi	22.1	nM	Ki	J Med Chem (2010) 53: 4511-4521 [PMID:20462211]
ChEMBL	Inhibition of [3H]WIN-35428 binding to human recombinant DAT expressed in CHO cells by scintillation counting	B	7.66	pKi	22.1	nM	Ki	J Med Chem (2009) 52: 5703-5711 [PMID:19722525]
ChEMBL	Displacement of [3H]-WIN-35428 from human DAT expressed in CHO cells	B	7.66	pKi	22.1	nM	Ki	J Med Chem (2011) 54: 6824-6831 [PMID:21916421]
GtoPdb	-	-	8	pKi	10	nM	Ki
ChEMBL	Inhibition of dopamine uptake in HEK cells expressing human dopamine transporter (hDAT)	F	7.37	pIC50	43	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Ability to displace [3H]WIN-35428 from dopamine transporter on guinea pig striatal membrane.	B	7.37	pIC50	42.6	nM	IC50	J Med Chem (2002) 45: 4110-4118 [PMID:12213054]
ChEMBL	Ability to displace [3H]WIN-35428 from Dopamine Transporter in guinea pig striatal membrane	F	7.37	pIC50	42.6	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Displacement of [3H]WIN-35428 form human DAT expressed in CHO cell membranes	B	7.66	pIC50	22.1	nM	IC50	Bioorg Med Chem Lett (2010) 20: 2809-2812 [PMID:20378347]
ChEMBL	Displacement of [3H]WIN-35428 from human recombinant DAT expressed in CHO cells	B	7.66	pIC50	22.1	nM	IC50	Bioorg Med Chem Lett (2008) 18: 6067-6070 [PMID:18951020]
ChEMBL	Inhibition of [3H]WIN-35428 binding to human recombinant DAT expressed in CHO cells	B	7.66	pIC50	22	nM	IC50	Bioorg Med Chem Lett (2009) 19: 2464-2467 [PMID:19329313]
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	7.89	pIC50	13	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
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	6.39	pKi	404	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	7.89	pIC50	13	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	Binding affinity to a single, sodium-dependent site on the Dopamine transporter in rat striatal membranes	B	8.06	pKd	8.63	nM	Kd	Bioorg Med Chem Lett (2000) 10: 1443-1446 [PMID:10888328]
ChEMBL	Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats	B	7.35	pKi	44.3	nM	Ki	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
ChEMBL	Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes	B	7.38	pKi	41.6	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL	Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes	B	7.49	pKi	32	nM	Ki	J Med Chem (1994) 37: 1535-1542 [PMID:8182712]
ChEMBL	Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter.	B	6.54	pIC50	290	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]dopamine uptake at the dopamine transporter.	B	7.07	pIC50	85	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]GBR-12935 binding to the dopamine transporter.	B	7.11	pIC50	77	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Compound was tested for inhibition of [3H]WIN-35428 binding at the dopamine transporter in rat striatal membrane	B	7.37	pIC50	42.6	nM	IC50	J Med Chem (1996) 39: 4935-4941 [PMID:8960553]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the dopamine transporter.	B	7.85	pIC50	14	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]BTCP binding to the dopamine transporter.	B	7.89	pIC50	13	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Ability to displace [3H]WIN-35428 from dopamine transporter on rat striatal membrane.	B	7.89	pIC50	12.94	nM	IC50	J Med Chem (2002) 45: 4110-4118 [PMID:12213054]
ChEMBL	Inhibition of [3H]cocaine binding to the dopamine transporter.	B	8.05	pIC50	9	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
ChEMBL	Inhibition of [3H]dopamine uptake at the dopamine transporter in rat striatal tissue	F	8.08	pIC50	8.4	nM	IC50	J Med Chem (1996) 39: 4935-4941 [PMID:8960553]
ChEMBL	Inhibition of [3H]WIN-35428 binding to the dopamine transporter in rat brain	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (1996) 39: 4935-4941 [PMID:8960553]
ChEMBL	Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (2002) 45: 4119-4127 [PMID:12213055]
ChEMBL	Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter.	B	8.15	pIC50	7	nM	IC50	J Med Chem (1992) 35: 969-981 [PMID:1552510]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells	B	7.74	pKi	18	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [125I]- RTI -55 binding at the Norepinephrine transporter sites on HEK-hNET cells	B	7.74	pKi	18	nM	Ki	J Med Chem (2002) 45: 4110-4118 [PMID:12213054]
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	7.87	pKi	13.5	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
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	7.95	pKi	11.3	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
GtoPdb	-	-	8.9	pKi	1.26	nM	Ki
ChEMBL	Inhibition of NE uptake in HEK cells expressing human noradrenaline transporter (hNET)	F	8.31	pIC50	4.9	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
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	9.04	pIC50	0.92	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity against 5-hydroxytryptamine 1A receptor (5-HT1A) by displacement of [3H]8-OH-DPAT from rat hippocampus membranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL	Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]-ketanserin from rat prefrontal cerebral cortex mambranes	B	6	pIC50	>1000	nM	IC50	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	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	6.87	pKi	136	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Displacement of [125I]- RTI-55 from Serotonin transporter expressed in HEK cells	B	7.3	pKi	50	nM	Ki	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
ChEMBL	Inhibition of [125I]- RTI -55 binding at the Serotonin transporter sites on HEK-hSERT cells	B	7.3	pKi	50	nM	Ki	J Med Chem (2002) 45: 4110-4118 [PMID:12213054]
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	7.35	pKi	45	nM	Ki	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
ChEMBL	Inhibition of 5-HT uptake in HEK cells expressing human serotonin transporter (hSERT)	F	7.03	pIC50	94	nM	IC50	J Med Chem (2002) 45: 4097-4109 [PMID:12213053]
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	7.27	pIC50	54	nM	IC50	J Med Chem (2017) 60: 3109-3123 [PMID:28319392]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats	B	6.61	pKi	247.5	nM	Ki	J Med Chem (2003) 46: 5512-5532 [PMID:14640559]
ChEMBL	Compound was tested for inhibition of [3H]5-HT reuptake at Serotonin transporter	B	6.64	pIC50	231	nM	IC50	J Med Chem (1996) 39: 4935-4941 [PMID:8960553]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	The compound was tested for affinity towards sigma-3 receptor	B	6.63	pIC50	234.42	nM	IC50	J Med Chem (1994) 37: 4109-4117 [PMID:7990111]

ChEMBL data shown on this page come from version 32:

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]