ChEMBL ligand: CHEMBL1059 (Alzain, Axalid, CI-1008, Lecaent, Lyrica, Lyrica cr, NSC-759256, PD-144723, Pregabalin, Pregabalin mylan, Pregabalin sandoz, Pregabalin sandoz gmbh, Pregabalin zentiva, Rewisca, Vronogabic, YNP-1807)
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
Voltage-dependent calcium channel alpha2delta subunit in Pig [ChEMBL: CHEMBL3985] [UniProtKB: O77773] There should be some charts here, you may need to enable JavaScript!
Voltage-gated calcium channel alpha2/delta subunit 1 in Human [ChEMBL: CHEMBL1919] [UniProtKB: P54289] There should be some charts here, you may need to enable JavaScript!
Voltage-gated calcium channel alpha2/delta subunit 2 in Human [ChEMBL: CHEMBL3896] [UniProtKB: Q9NY47] 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]
ChEMBL	Displacement of [3H]-nisoxetine from human NET expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method	B	5	pKi	>10000	nM	Ki	J Med Chem (2021) 64: 2167-2185 [PMID:33591743]
ChEMBL	Inhibition of human NET expressed in HEK293 cells assessed as reduction in ASP+ uptake incubated for 20 mins before ASP+ addition and measured after 90 mins by scintillation counting method	B	5	pIC50	>10000	nM	IC50	J Med Chem (2021) 64: 2167-2185 [PMID:33591743]
Voltage-dependent calcium channel alpha2delta subunit in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3985] [UniProtKB: O77773]
ChEMBL	Displacement of [3H]gabapentin from calcium channel alpha2delta in pig cerebral cortex membrane after 30 mins	B	7.1	pIC50	80	nM	IC50	Bioorg Med Chem Lett (2010) 20: 362-365 [PMID:19897364]
ChEMBL	Displacement of [3H]gabapentin from alpha-2delta calcium channel in pig brain membrane	B	7.14	pIC50	73	nM	IC50	Bioorg Med Chem Lett (2006) 16: 2329-2332 [PMID:16099652]
Voltage-gated calcium channel alpha2/delta subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1919] [UniProtKB: P54289]
ChEMBL	Displacement of [3H]-gabapentin from human Cav alpha2delta1 expressed in CHO-K1 cell membranes incubated for 60 mins by scintillation counting method	B	7.72	pKi	19	nM	Ki	J Med Chem (2021) 64: 2167-2185 [PMID:33591743]
ChEMBL	Displacement of [3H]-gabapentin from human Cav alpha2delta1 expressed in CHO-K1 cell membranes incubated for 60 mins by scintillation counting method	B	7.72	pKi	19	nM	Ki	ACS Med Chem Lett (2021) 12: 1802-1809 [PMID:34795870]
Voltage-gated calcium channel alpha2/delta subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3896] [UniProtKB: Q9NY47]
ChEMBL	Displacement of [3H]-gabapentin from human Cav alpha2delta2 expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method	B	7	pKi	99	nM	Ki	J Med Chem (2021) 64: 2167-2185 [PMID:33591743]

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]