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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 |
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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 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]