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, Dextrostat, Ferndex, NSC-73713, Xelstrym)
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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 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 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]