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!
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975] 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]
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975]
ChEMBL	Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay	B	4.85	pIC50	14000	nM	IC50	RSC Med Chem (2022) 13: 183-195 [PMID:35308021]
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 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]