dexamfetamine [Ligand Id: 2147] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL612 (Amfetamine, (s)-, Amphetamine, d-, D-amphetamine, Dexamfetamine, Dexampex, Dexamphetamine, Dexedrine, Dexidrine, Dextroamphetamine, Dextroamphetamine resin complex, Dextrostat, Ferndex, NSC-73713, Xelstrym) |
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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] | ||||||||
| GtoPdb | - | - | 6.96 | pKi | 109 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-5 [PMID:23602445] |
| 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 | 6.96 | pKi | 109 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| 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 | 6.54 | pIC50 | 288.4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| ChEMBL | Inhibition of [3H]dopamine reuptake at human DAT cloned in rat brain synaptosome by scintillation counting | B | 7.61 | pEC50 | 24.8 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Nat Prod (1995) 58: 1475-1484 [PMID:8676127] |
| ChEMBL | Activity at DAT in rat synaptosomes assessed as release of [3H]DA after 5 mins by liquid scintillation counting method | B | 7.6 | pEC50 | 25 | nM | EC50 | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| ChEMBL | Activity at DAT in rat synaptosomes obtained from striatum assessed as release of [3H]MPP+ by liquid scintillation counting method | B | 7.61 | pEC50 | 24.8 | nM | EC50 | Medchemcomm (2016) 7: 1657-1663 |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Inhibition of human recombinant MAOA by spectrophotometrically | B | 4.84 | pKi | 14400 | nM | Ki | Bioorg Med Chem (2010) 18: 1388-1395 [PMID:20123154] |
| Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
| ChEMBL | Inhibition of MAOA in rat brain mitochondrial suspension | B | 4.91 | pKi | 12200 | nM | Ki | Bioorg Med Chem (2010) 18: 1388-1395 [PMID:20123154] |
| Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | Inhibition of MAOB in rat brain mitochondrial suspension | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem (2010) 18: 1388-1395 [PMID:20123154] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| 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 | 7 | pKi | 101 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| GtoPdb | - | - | 7 | pKi | 101 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-5 [PMID:23602445] |
| 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 | 6.2 | pIC50 | 630.96 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| ChEMBL | Inhibition of [3H]norepinephrine reuptake at human NET cloned in rat brain synaptosome by scintillation counting | B | 8.15 | pEC50 | 7.1 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| 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 | 5.24 | pKi | 5728 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| 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 | 4.78 | pIC50 | 16595.87 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445] |
| ChEMBL | Inhibition of [3H]5-HT uptake at human SERT cloned in rat brain synaptosome by scintillation counting | B | 5.75 | pEC50 | 1770 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Activity at SERT in rat synaptosomes obtained from whole brain minus striatum and cerebellum assessed as release of [3H]5-HT by liquid scintillation counting method | B | 5.75 | pEC50 | 1770 | nM | EC50 | Medchemcomm (2016) 7: 1657-1663 |
| ChEMBL | Activity at SERT in rat synaptosomes assessed as release of [3H]HT after 5 mins by liquid scintillation counting method | B | 5.75 | pEC50 | 1765 | nM | EC50 | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| Trace amine-associated receptor 1 in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926495] [UniProtKB: Q8HZ64] | ||||||||
| ChEMBL | Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader | F | 6 | pEC50 | 1010 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] | ||||||||
| ChEMBL | Activation of human TAAR1 expressed in Syrian hamster AV12-664 cells co-expressing GalphaS protein assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method in presence of RX821002 and alprenolol | F | 6 | pEC50 | 990 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| ChEMBL | Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay | F | 6.03 | pEC50 | 935 | nM | EC50 | Bioorg Med Chem (2008) 16: 7415-7423 [PMID:18602830] |
| ChEMBL | Activation of C-terminal HA epitope tagged human TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein, Galpha16 by cAMP accumulation assay | F | 6.22 | pEC50 | 600 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| ChEMBL | Activation of human TAAR1 expressed in human HEK293T cells assessed as cAMP accumulation after 10 mins by BRET assay | F | 6.85 | pEC50 | 140 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| GtoPdb | - | - | 6.9 | pEC50 | - | - | - |
Mol Pharmacol (2008) 74: 585-594 [PMID:18524885]; Bioorg Med Chem (2011) 19: 7044-8 [PMID:22037049] |
| TA1 receptor/Trace amine-associated receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8] | ||||||||
| ChEMBL | Activation of mouse TAAR1 transmembrane domain 7 Tyr287(7.39)Asn mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 6.66 | pEC50 | 218.8 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
| ChEMBL | Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting | F | 6.68 | pEC50 | 210 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| ChEMBL | Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 7.07 | pEC50 | 84.6 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
| ChEMBL | Activation of mouse TAAR1 transmembrane domain 6 Thr268(6.55)Met mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 8.4 | pEC50 | 3.98 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
| ChEMBL | Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| GtoPdb | - | - | 8.7 | pEC50 | - | - | - |
J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486]; Genes Brain Behav (2007) 6: 628-39 [PMID:17212650] |
| TA1 receptor/Trace amine-associated receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9] | ||||||||
| ChEMBL | Activation of rat TAAR1 expressed in Syrian hamster AV12-664 cells assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method | F | 5.92 | pEC50 | 1200 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| ChEMBL | Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting | F | 6.09 | pEC50 | 810 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| ChEMBL | Activation of rat TAAR1 transmembrane domain 6 Met268(6.55)Thr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 6.17 | pEC50 | 677.4 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
| ChEMBL | Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by competitive binding assay | F | 6.36 | pEC50 | 440 | nM | EC50 | Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049] |
| GtoPdb | - | - | 6.4 | pEC50 | - | - | - |
J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486]; Mol Pharmacol (2001) 60: 1181-8 [PMID:11723224] |
| ChEMBL | Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 7.25 | pEC50 | 55.6 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
| ChEMBL | Activation of rat TAAR1 transmembrane domain 7 Asn287(7.39)Tyr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay | F | 7.86 | pEC50 | 13.9 | nM | EC50 | J Med Chem (2014) 57: 378-390 [PMID:24354319] |
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]
