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, Dexanfetamina, 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 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]
