ChEMBL ligand: CHEMBL668 (Protriptyline)
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
SERT in Human [GtoPdb: 928] [UniProtKB: P31645] 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
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
GtoPdb	-	-	8.85	pKd	1.41	nM	Kd	Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]
ChEMBL	Inhibition of human NET	B	8.85	pKd	1.4	nM	Kd	J Med Chem (2010) 53: 7869-7873 [PMID:20945906]
ChEMBL	Displacement of radiolabeled protriptyline from human NET	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
GtoPdb	-	-	8.17	pKi	6.8	nM	Ki	J Med Chem (2008) 51: 7094-8 [PMID:18983139]
ChEMBL	Displacement of [3H]nisoxetine from human NE transporter	B	8.64	pKi	2.3	nM	Ki	J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL	Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells after 120 mins by scintillation counting	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL	Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting	B	8.7	pKi	2	nM	Ki	J Med Chem (2012) 55: 3488-3501 [PMID:22420844]
ChEMBL	Binding affinity to human norepinephrine transporter by radioligand displacement assay	B	8.8	pKi	1.6	nM	Ki	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Inhibition of human aorepinephrine transporter	B	7.77	pIC50	17	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	Displacement of radiolabeled protriptyline from human NET	B	8.04	pIC50	9.1	nM	IC50	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Inhibition of human NET	B	8.15	pIC50	7.1	nM	IC50	J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL	Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells after 120 mins by scintillation counting	B	8.54	pIC50	2.9	nM	IC50	J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL	Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells	B	8.55	pIC50	2.8	nM	IC50	Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL	Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method	B	8.55	pIC50	2.8	nM	IC50	Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL	Binding affinity to human nonepinephrine transporter by radioligand displacement assay	B	8.6	pIC50	2.5	nM	IC50	Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL	Binding affinity to human norepinephrine transporter by radioligand displacement assay	B	8.68	pIC50	2.1	nM	IC50	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of [3H]nisoxetine from human NET expressed in CHO cells after 120 mins by scintillation counting	B	8.77	pIC50	1.7	nM	IC50	J Med Chem (2012) 55: 3488-3501 [PMID:22420844]
GtoPdb	Inhibition of [3H]nisoxetine binding to CHO cells expressing hNET.	-	8.77	pIC50	1.7	nM	IC50	J Med Chem (2012) 55: 3488-501 [PMID:22420844]
ChEMBL	Percent inhibition against Norepinephrine transporter at 1 uM nonselective	B	8.96	pIC50	1.1	nM	IC50	J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
SERT in Human [GtoPdb: 928] [UniProtKB: P31645]
GtoPdb	-	-	7.71	pKd	19.6	nM	Kd	Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821]

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]