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

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ChEMBL ligand: CHEMBL1446457
  • BGT1/Betaine transporter in Human [ChEMBL: CHEMBL3715] [GtoPdb: 932] [UniProtKB: P48065]
  • BGT1 in Mouse [GtoPdb: 932] [UniProtKB: P31651]
  • This target only has 1 pki data point
  • 5.9
1 CHEMBL1446457_lig_chart_1 Betaine transporter HumanMouse
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  • GAT1/GABA transporter 1 in Human [ChEMBL: CHEMBL1903] [GtoPdb: 929] [UniProtKB: P30531]
  • GAT1/GABA transporter 1 in Mouse [ChEMBL: CHEMBL5445] [GtoPdb: 929] [UniProtKB: P31648]
  • This target only has 1 pki data point
  • 4.72
2 CHEMBL1446457_lig_chart_2 GABA transporter 1 HumanMouse
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3 CHEMBL1446457_lig_chart_3 GABA transporter 2 HumanMouse
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  • GAT3/GABA transporter 3 in Human [ChEMBL: CHEMBL5208] [GtoPdb: 931] [UniProtKB: P48066]
  • GAT2/GABA transporter 3 in Mouse [ChEMBL: CHEMBL5205] [GtoPdb: 930] [UniProtKB: P31649]
  • This target only has 1 pki data point
  • 4.39
4 CHEMBL1446457_lig_chart_4 GABA transporter 3 HumanMouse
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  • GAT3/GABA transporter 4 in Mouse [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650]
  • This target only has 1 pki data point
  • 4.82
5 CHEMBL1446457_lig_chart_5 GABA transporter 4 Mouse
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]