mazindol [Ligand Id: 4797] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL781 (42-548, AN-448, Magrilon, Mazanor, Mazildene, Mazindol, Mazindol civ, SAH-42548, Sanorex, Terenac, Teronac) |
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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] |
| 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 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]
