dexamfetamine [Ligand Id: 2147] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL612 (Dextroamphetamine, Dexampex, Dexamfetamine, Dexedrine, d-Amphetamine, Dextrostat, Ferndex, Dextroamphetamine resin complex, Dexamphetamine)
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • Trace amine-associated receptor 1 in Rhesus macaque [ChEMBL: CHEMBL1926495] [UniProtKB: Q8HZ64]
  • TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
  • TA1 receptor/Trace amine-associated receptor 1 in Mouse [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8]
  • TA1 receptor/Trace amine-associated receptor 1 in Rat [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9]
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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 B 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 expressed in human HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting B 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 B 7.07 pEC50 84.6 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 B 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: 178-186 [PMID:17218486];
Genes Brain Behav (2007) 6: 628-639 [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 B 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 B 6.09 pEC50 810 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 competitive binding assay B 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: 178-186 [PMID:17218486];
Mol Pharmacol (2001) 60: 1181-1188 [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 B 7.25 pEC50 55.6 nM EC50 J. Med. Chem. (2014) 57: 378-390 [PMID:24354319]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]