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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
