ChEMBL ligand: CHEMBL43048 (3,4-methylenedioxymetamphetamine, 3,4-methylenedioxymethamphetamine, Ecstasy, Mdma, Methylenedioxymetamphetamine, Methylenedioxymethamfetamine, Methylenedioxymethamphetamine, Methylenedioxy Methamphetamine, Midomafetamine)
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!
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390] 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!
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]
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	6.05	pKi	897	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	5.62	pIC50	2398.83	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of human dopamine transporter	B	5.84	pIC50	1442	nM	IC50	Eur J Med Chem (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL	Binding affinity to human DAT	B	5.84	pIC50	1442	nM	IC50	Bioorg Med Chem (2010) 18: 4009-4031 [PMID:20466553]
ChEMBL	Binding affinity to human DAT expressed in HEK293 cells assessed as induction of [3H]MPP+ release by liquid scintillation counting method	B	6	pEC50	1000	nM	EC50	Bioorg Med Chem (2015) 23: 5574-5579 [PMID:26233799]
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Activity at DAT in rat synaptosomes assessed as release of [3H]DA after 5 mins by liquid scintillation counting method	B	6.56	pEC50	278	nM	EC50	J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL	Binding affinity to DAT in Sprague-Dawley rat brain synaptosomes assessed as induction of [3H]MPP+ release by liquid scintillation counting method	B	7.12	pEC50	75	nM	EC50	Bioorg Med Chem (2015) 23: 5574-5579 [PMID:26233799]
nicotinic acetylcholine receptor α4 subunit/nicotinic acetylcholine receptor β2 subunit/Neuronal acetylcholine receptor; alpha4/beta2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907596] [GtoPdb: 465, 472] [UniProtKB: P09483, P12390]
ChEMBL	Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat brain cortical membrane after 3 hrs	B	5.84	pKi	1440	nM	Ki	Eur J Med Chem (2014) 81: 35-46 [PMID:24942641]
ChEMBL	Displacement of [3H]epibatidine from alpha4beta2 nAChR in Sprague-Dawley rat brain cortical membrane after 3 hrs by liquid scintillation spectrometric analysis	B	4.52	pIC50	30400	nM	IC50	Eur J Med Chem (2014) 81: 35-46 [PMID:24942641]
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	6.4	pKi	398	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [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	5.7	pIC50	1995.26	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of human noradrenaline transporter	B	6.39	pIC50	405	nM	IC50	Eur J Med Chem (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL	Binding affinity to human NET	B	6.39	pIC50	405	nM	IC50	Bioorg Med Chem (2010) 18: 4009-4031 [PMID:20466553]
ChEMBL	Binding affinity to human NET expressed in HEK293 cells assessed as induction of [3H]MPP+ release by liquid scintillation counting method	B	6	pEC50	1000	nM	EC50	Bioorg Med Chem (2015) 23: 5574-5579 [PMID:26233799]
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	6.02	pKi	948	nM	Ki	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Displacement of [3H]paroxetine from human SERT expressed in HEK293 cells	B	8.69	pKi	2.03	nM	Ki	Bioorg Med Chem (2008) 16: 6364-6370 [PMID:18487050]
ChEMBL	Displacement of [3H]citalopram from human SERT expressed in HEK293 cells	B	9.14	pKi	0.73	nM	Ki	Bioorg Med Chem (2008) 16: 6364-6370 [PMID:18487050]
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	5.56	pIC50	2754.23	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3411-3415 [PMID:23602445]
ChEMBL	Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay	B	5.96	pIC50	1100	nM	IC50	Bioorg Med Chem (2011) 19: 1328-1348 [PMID:21227702]
ChEMBL	Inhibition of [3H]5-HT uptake at SERT	B	6.37	pIC50	425	nM	IC50	Eur J Med Chem (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL	Binding affinity to human SERT	B	6.37	pIC50	425	nM	IC50	Bioorg Med Chem (2010) 18: 4009-4031 [PMID:20466553]
ChEMBL	Induction of human SERT-dependent cytotoxicity in SERT expressing human DG75 cells after 48 hrs by neutral red assay	B	4.49	pEC50	32359.37	nM	EC50	Eur J Med Chem (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL	Binding affinity to human SERT expressed in HEK293 cells assessed as induction of [3H]5-HT release by liquid scintillation counting method	B	6	pEC50	1000	nM	EC50	Bioorg Med Chem (2015) 23: 5574-5579 [PMID:26233799]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting	B	5.97	pIC50	1060	nM	IC50	Eur J Med Chem (2009) 44: 4862-4888 [PMID:19717215]
ChEMBL	Activity at SERT in rat synaptosomes assessed as release of [3H]HT after 5 mins by liquid scintillation counting method	B	7.14	pEC50	72	nM	EC50	J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL	Binding affinity to SERT in Sprague-Dawley rat brain synaptosomes assessed as induction of [3H]5-HT release by liquid scintillation counting method	B	7.21	pEC50	61	nM	EC50	Bioorg Med Chem (2015) 23: 5574-5579 [PMID:26233799]
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 HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by competitive binding assay	F	5.77	pEC50	1700	nM	EC50	Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]

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]