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 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]