NNC052090 [Ligand Id: 4610] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1446457
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BGT1/Betaine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3715] [GtoPdb: 932] [UniProtKB: P48065]
ChEMBL Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis B 5.29 pIC50 5100 nM IC50 Bioorg Med Chem (2013) 21: 4938-4950 [PMID:23886812]
ChEMBL Inhibition of human BGT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis B 5.29 pIC50 5100 nM IC50 ACS Med Chem Lett (2014) 5: 889-893 [PMID:25147609]
BGT1 in Mouse [GtoPdb: 932] [UniProtKB: P31651]
GtoPdb - - 5.9 pKi 1400 nM Ki Br J Pharmacol (1997) 120: 983-5 [PMID:9134205]
GAT1/GABA transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
ChEMBL Inhibition of human GAT1 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis B 4.94 pIC50 11400 nM IC50 ACS Med Chem Lett (2014) 5: 889-893 [PMID:25147609]
GAT1/GABA transporter 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
ChEMBL Inhibition of mouse GAT1 expressed in hamster BHK cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.72 pKi 19000 nM Ki J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in BHK cells B 4.72 pIC50 19054.61 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
ChEMBL Inhibition of mouse mGAT1 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis B 4.72 pIC50 19000 nM IC50 Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526]
ChEMBL Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells B 4.99 pIC50 10232.93 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
GAT2/GABA transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4535] [GtoPdb: 930] [UniProtKB: Q9NSD5]
ChEMBL Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis B 5.21 pIC50 6200 nM IC50 ACS Med Chem Lett (2014) 5: 889-893 [PMID:25147609]
BGT1/GABA transporter 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4228] [GtoPdb: 932] [UniProtKB: P31651]
ChEMBL Inhibition of mouse BGT1 expressed in hamster BHK cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 5.85 pKi 1400 nM Ki J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
GtoPdb - - 5.9 pKi 1400 nM Ki Br J Pharmacol (1997) 120: 983-5 [PMID:9134205]
ChEMBL Inhibition of mouse mGAT2 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis B 5.85 pIC50 1400 nM IC50 Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526]
GAT3/GABA transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5208] [GtoPdb: 931] [UniProtKB: P48066]
ChEMBL Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis B 5.05 pIC50 8920 nM IC50 ACS Med Chem Lett (2014) 5: 889-893 [PMID:25147609]
GAT2/GABA transporter 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5205] [GtoPdb: 930] [UniProtKB: P31649]
ChEMBL Inhibition of mouse GAT2 expressed in hamster BHK cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.39 pKi 41000 nM Ki J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of mouse mGAT3 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis B 4.39 pIC50 41000 nM IC50 Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526]
ChEMBL Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells B 5.09 pIC50 8128.31 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
ChEMBL Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in BHK cells B 5.85 pIC50 1412.54 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
GAT3/GABA transporter 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650]
ChEMBL Inhibition of mouse GAT3 expressed in hamster BHK cells assessed as reduction in [3H]GABA uptake after 3 mins by scintillation counting method B 4.82 pKi 15000 nM Ki J Med Chem (2017) 60: 8834-8846 [PMID:28991462]
ChEMBL Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in BHK cells B 4.39 pIC50 40738.03 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
ChEMBL Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in BHK cells B 4.82 pIC50 15135.61 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]
ChEMBL Inhibition of mouse mGAT4 expressed in HEK293 cells assessed as inhibition of [3H]GABA uptake after 3 mins incubation by TopCount microplate scintillation counting analysis B 4.82 pIC50 15000 nM IC50 Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526]
ChEMBL Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells B 4.93 pIC50 11748.98 nM IC50 Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173]

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]