ChEMBL ligand: CHEMBL612 (Amfetamine, (s)-, Amphetamine, d-, D-amphetamine, Dexamfetamine, Dexampex, Dexamphetamine, Dexedrine, Dexidrine, Dextroamphetamine, Dextroamphetamine resin complex, Dextrostat, Ferndex, NSC-73713)
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] DAT/Dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] Monoamine oxidase A in Rat [ChEMBL: CHEMBL3358] [UniProtKB: P21396] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase B in Rat [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!

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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]