[3H]mazindol [Ligand Id: 4591] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL781 (42-548, Mazindol, SAH-42548, Teronac, Mazindol civ, Sanorex, AN-448, Mazanor)
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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]
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]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]