ChEMBL ligand: CHEMBL1373 (CEP 1538, CEP-1538, CRC-40476, CRL 40476, CRL-40476, DEP-1538, Modafinil, Modafinil civ, MODAFINIL COMPONENT OF THN-102, MODAFINIL COMPONENT OF THN102, Modafinilo, Modaphonil, Modiodal, NSC-751178, NSC-759110, Provigil)
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] There should be some charts here, you may need to enable JavaScript!
Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] DAT/Sodium-dependent dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
SERT/Sodium-dependent serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
Transporter in Rat [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] 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
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]-N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method	B	4	pKi	>100000	nM	Ki	Eur J Med Chem (2020) 208: 112674-112674 [PMID:32947229]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Displacement of [3H]-N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method	B	4.41	pKi	39000	nM	Ki	Eur J Med Chem (2020) 208: 112674-112674 [PMID:32947229]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method	B	4	pKi	>100000	nM	Ki	Eur J Med Chem (2020) 208: 112674-112674 [PMID:32947229]
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
ChEMBL	Inhibition of high affinity uptake by the norepinephrine transporter from rat synaptosomal nerve endings by using [3H]NE as radioligand	B	5	pKi	>10000	nM	Ki	J Med Chem (2004) 47: 5821-5824 [PMID:15537337]
ChEMBL	Inhibition of rat brain NET assessed as reduction of [3H]-NE re-uptake preincubated for 30 mins followed by [3H]-NE addition measured after 5 mins by scintillation counting	B	5	pIC50	>10000	nM	IC50	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL	Binding affinity to wild type human DAT expressed in African green monkey COS7 cells assessed as inhibition of [3H]-dopamine uptake after 5 mins by beta-scintillation counting analysis	B	4.89	pKi	13000	nM	Ki	J Med Chem (2014) 57: 1000-1013 [PMID:24494745]
ChEMBL	Binding affinity to human DAT A480T mutant expressed in African green monkey COS7 cells assessed as inhibition of [3H]-dopamine uptake after 5 mins by beta-scintillation counting analysis	B	5.51	pKi	3090	nM	Ki	J Med Chem (2014) 57: 1000-1013 [PMID:24494745]
ChEMBL	Binding affinity to DAT (unknown origin)	B	5.7	pKi	2000	nM	Ki	J Med Chem (2016) 59: 10676-10691 [PMID:27933960]
ChEMBL	DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.84	pKi	1456	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Displacement of [3H]WIN35,428 from wild type human DAT expressed in COS7 cell membranes incubated for >90 mins by radioligand binding assay	B	6.03	pKi	927	nM	Ki	J Med Chem (2016) 59: 10676-10691 [PMID:27933960]
ChEMBL	Inhibition of re-uptake of [3H]-dopamine at human DAT expressed in HEK293 cells preincubated for 5 mins followed by [3H]-dopamine addition measured after 1 min by liquid scintillation counting	B	4.94	pIC50	11500	nM	IC50	J Med Chem (2017) 60: 9330-9348 [PMID:29091428]
ChEMBL	DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.74	pIC50	1832	nM	IC50	DrugMatrix in vitro pharmacology data
DAT/Sodium-dependent dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977]
ChEMBL	Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat striatum membranes incubated for 120 mins by microbeta scintillation counting method	B	5.09	pKi	8160	nM	Ki	J Med Chem (2020) 63: 2343-2357 [PMID:31661268]
ChEMBL	Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat striatal membranes incubated for 120 mins by microbeta scintillation counting method	B	5.09	pKi	8160	nM	Ki	Eur J Med Chem (2020) 208: 112674-112674 [PMID:32947229]
GtoPdb	Inhibition of high affinity uptake by the dopamine transporter from rat synaptosomal nerve endings using [3H]dopamine as radioligand	-	5.42	pKi	3800	nM	Ki	J Med Chem (2004) 47: 5821-4 [PMID:15537337]
ChEMBL	Inhibition of high affinity uptake by the dopamine transporter from rat synaptosomal nerve endings by using [3H]DA as radioligand	B	5.42	pKi	3800	nM	Ki	J Med Chem (2004) 47: 5821-5824 [PMID:15537337]
ChEMBL	Displacement of [3H]WIN35,428 from Sprague-Dawley rat brain DAT after 120 mins by liquid scintillation counting analysis	B	5.59	pKi	2600	nM	Ki	J Med Chem (2014) 57: 1000-1013 [PMID:24494745]
ChEMBL	Displacement of [3H]WIN35428 from DAT in Sprague-Dawley rat brain membranes	B	5.6	pKi	2520	nM	Ki	ACS Med Chem Lett (2011) 2: 48-52 [PMID:21344069]
ChEMBL	Dopamine Transporter Binding Assay: Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs) were removed, striatum dissected and quickly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of ice cold modified sucrose phosphate buffer (0.32 M sucrose, 7.74 mM Na2HPO4, 2.26 mM NaH2PO4, pH adjusted to 7.4) using a Brinkman Polytron (setting 6 for 20 sec) and centrifuged at 20,000ug for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 10 mg/ml. Ligand binding experiments were conducted in assay tubes containing 0.5 ml sucrose phosphate buffer for 120 min on ice. Each tube contained 0.5 nM 3H WIN 35428 (specific activity 84 Ci/mmol) and 1.0 mg striatal tissue (original wet weight). Nonspecific binding was determined using 0.1 mM cocaine HCl. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% PEI (polyethyleneimine), using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 5 ml cold buffer and transferred to scintillation vials.	B	5.6	pKi	2520	nM	Ki	US-9862679-B2. Potent and selective inhibitors of monoamine transporters; method of making; and use thereof (2018)
ChEMBL	Binding Assay: Dopamine Transporter Binding Assay. Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs) were removed, striatum dissected and quickly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of ice cold modified sucrose phosphate buffer (0.32 M sucrose, 7.74 mM Na2HPO4, 2.26 mM NaH2PO4, pH adjusted to 7.4) using a Brinkman Polytron (setting 6 for 20 sec) and centrifuged at 20,000×g for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 10 mg/ml. Ligand binding experiments were conducted in assay tubes containing 0.5 ml sucrose phosphate buffer for 120 min on ice. Each tube contained 0.5 nM 3H WIN 35428 (specific activity 84 Ci/mmol) and 1.0 mg striatal tissue (original wet weight). Nonspecific binding was determined using 0.1 mM cocaine HCl. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% PEI (polyethyleneimine), using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 5 ml cold buffer and transferred to scintillation vials. Beckman Ready Safe (3.0 ml) was added and the vials were counted the next day using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.). Data were analyzed by using GraphPad Prism software (San Diego, Calif.).	B	5.6	pKi	2520	nM	Ki	US-10913711-B2. Potent and selective inhibitors of monoamine transporters; method of making; and use thereof (2021)
ChEMBL	Dopamine Transporter Binding Assay: Dopamine Transporter Binding Assay. Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs) were removed, striatum dissected and quickly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of ice cold modified sucrose phosphate buffer (0.32 M sucrose, 7.74 mM Na2HPO4, 2.26 mM NaH2PO4, pH adjusted to 7.4) using a Brinkman Polytron (setting 6 for 20 sec) and centrifuged at 20,000×g for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 10 mg/ml. Ligand binding experiments were conducted in assay tubes containing 0.5 ml sucrose phosphate buffer for 120 min on ice. Each tube contained 0.5 nM 3H WIN 35428 (specific activity 84 Ci/mmol) and 1.0 mg striatal tissue (original wet weight). Nonspecific binding was determined using 0.1 mM cocaine HCl. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% PEI (polyethyleneimine), using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 5 ml cold buffer and transferred to scintillation vials. Beckman Ready Safe (3.0 ml) was added and the vials were counted the next day using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.). Data were analyzed by using GraphPad Prism software (San Diego, Calif.).	B	5.6	pKi	2520	nM	Ki	US-11555013-B2. Potent and selective inhibitors of monoamine transporters; method of making; and use thereof (2023)
ChEMBL	Inhibition of rat DAT-mediated dopamine reuptake	B	5.37	pIC50	4300	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2312-2314 [PMID:22264475]
ChEMBL	Inhibition of rat DAT-mediated dopamine reuptake	B	5.37	pIC50	4300	nM	IC50	Eur J Med Chem (2012) 54: 949-951 [PMID:22749190]
ChEMBL	Inhibition of rat brain DAT assessed as reduction of [3H]-DA re-uptake preincubated for 30 mins followed by [3H]-DA addition measured after 5 mins by scintillation counting	B	5.42	pIC50	>3800	nM	IC50	J Med Chem (2018) 61: 2133-2165 [PMID:28731336]
ChEMBL	Inhibition of rat DAT	B	5.43	pIC50	3700	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2312-2314 [PMID:22264475]
ChEMBL	Displacement of 3H-WIN-35428 from DAT in rat striata after 120 mins	B	5.43	pIC50	3700	nM	IC50	Bioorg Med Chem Lett (2012) 22: 3751-3753 [PMID:22546675]
ChEMBL	Inhibition of rat DAT	B	5.43	pIC50	3700	nM	IC50	Eur J Med Chem (2012) 54: 949-951 [PMID:22749190]
SERT/Sodium-dependent serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Displacement of [3H]citalopram from SERT in Sprague-Dawley rat midbrain membranes incubated for 60 mins by microbeta scintillation counting method	B	4.5	pKi	31300	nM	Ki	J Med Chem (2020) 63: 2343-2357 [PMID:31661268]
ChEMBL	Displacement of [3H]citalopram from SERT in Sprague-Dawley rat midbrain membranes incubated for 60 mins by microbeta scintillation counting method	B	4.5	pKi	31300	nM	Ki	Eur J Med Chem (2020) 208: 112674-112674 [PMID:32947229]
Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380]
ChEMBL	Inhibition of rat NET-mediated norepinephrine reuptake	B	4.19	pIC50	63900	nM	IC50	Bioorg Med Chem Lett (2012) 22: 2312-2314 [PMID:22264475]
ChEMBL	Inhibition of rat NET-mediated norepinephrine reuptake	B	4.19	pIC50	63900	nM	IC50	Eur J Med Chem (2012) 54: 949-951 [PMID:22749190]

ChEMBL data shown on this page come from version 36:

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]