SNAP-5114 [Ligand Id: 4677] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL75035 (SNAP-5114) |
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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 | 4.14 | pIC50 | 71700 | 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 | 4.14 | pIC50 | 71700 | nM | IC50 | ACS Med Chem Lett (2014) 5: 889-893 [PMID:25147609] |
| 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 | pIC50 | >100000 | 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 | Binding affinity to mouse GAT1 stably transfected in HEK293 cells by NO-711 binding assay | B | 4.56 | pKi | 27542.29 | nM | Ki | Bioorg Med Chem (2013) 21: 5154-5167 [PMID:23859778] |
| ChEMBL | Displacement of NO711 from mouse GAT1 expressed in HEK293 cells by LC-MS/MS analysis | B | 4.56 | pKi | 27542.29 | nM | Ki | Eur J Med Chem (2014) 83: 256-273 [PMID:24973660] |
| ChEMBL | Inhibition of [2H10]NO 711 binding to mouse GAT1 expressed in HEK293 cell membranes after 40 mins by LC-ESI-MS-MS analysis | B | 4.56 | pKi | 27542.29 | nM | Ki | Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082] |
| ChEMBL | Inhibition of mouse GAT1 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Eur J Med Chem (2021) 221: 113512-113512 [PMID:34015586] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| ChEMBL | Inhibition of [3H]GABA uptake at mouse GAT1 expressed in HEK cells | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300] |
| ChEMBL | Inhibition of GABA uptake at murine GAT-1 expressed in HEK293 cells | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Eur J Med Chem (2013) 65: 487-499 [PMID:23770450] |
| ChEMBL | Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cells | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Bioorg Med Chem (2013) 21: 5154-5167 [PMID:23859778] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Eur J Med Chem (2014) 83: 256-273 [PMID:24973660] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK293 cells by [3H]GABA uptake assay | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition measured after 4 mins by liquid scintillation counting analysis | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082] |
| ChEMBL | Inhibition of mouse GAT1 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting analysis | B | 4.07 | pIC50 | 85113.8 | nM | IC50 | Bioorg Med Chem (2019) 27: 144-152 [PMID:30503411] |
| ChEMBL | Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells | B | 4.07 | pIC50 | 85000 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| 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 | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526] |
| 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 | 4.92 | pIC50 | 11900 | nM | IC50 | Bioorg Med Chem (2013) 21: 4938-4950 [PMID:23886812] |
| ChEMBL | Inhibition of human GAT2 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | B | 4.92 | pIC50 | 11900 | 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 GABA uptake at murine BGT-1 expressed in HEK293 cells | B | 4.51 | pIC50 | 30902.95 | nM | IC50 | Eur J Med Chem (2013) 65: 487-499 [PMID:23770450] |
| 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 | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526] |
| GAT2/GABA transporter 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4889] [GtoPdb: 930] [UniProtKB: P31646] | ||||||||
| ChEMBL | Inhibitory activity against rat GABA transporter-2 (rGAT2) | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (1994) 37: 2334-2342 [PMID:8057281] |
| ChEMBL | Inhibition of rat GAT2 assessed as [3H]GABA uptake | B | 4.68 | pIC50 | 20892.96 | nM | IC50 | Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173] |
| GtoPdb | - | - | 4.7 | pIC50 | 20000 | nM | IC50 | Recept Channels (1994) 2: 207-13 [PMID:7874447] |
| GAT3/GABA transporter 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5208] [GtoPdb: 931] [UniProtKB: P48066] | ||||||||
| ChEMBL | Inhibition of human GAT3 assessed as [3H]GABA uptake | B | 5.3 | pIC50 | 5011.87 | nM | IC50 | Bioorg Med Chem (2011) 19: 6492-6504 [PMID:21940173] |
| ChEMBL | Inhibitory activity against human sodium and chloride dependent GABA transporter 3 | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1994) 37: 2334-2342 [PMID:8057281] |
| ChEMBL | Binding affinity to GAT3 | B | 5.3 | pIC50 | 5000 | nM | IC50 | Eur J Med Chem (2010) 45: 2453-2466 [PMID:20219271] |
| ChEMBL | Inhibition of human GAT3 expressed in COS7 cells assessed as reduction in [2H6]GABA uptake preincubated for 25 mins followed by [2H6]GABA addition and measured after 6 mins by LC-MS/MS analysis | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem (2019) 27: 144-152 [PMID:30503411] |
| ChEMBL | Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | B | 5.95 | pIC50 | 1120 | nM | IC50 | Bioorg Med Chem (2013) 21: 4938-4950 [PMID:23886812] |
| ChEMBL | Inhibition of human GAT3 transfected in CHO cells assessed as [3H]GABA uptake after 20 mins by liquid scintillation counting analysis | B | 5.95 | pIC50 | 1120 | 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-mediated [3H]GABA uptake expressed in human HEK cells | B | 4.46 | pIC50 | 35000 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| ChEMBL | Inhibition of mouse GAT2 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | B | 4.66 | pIC50 | 21900 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 417-423 [PMID:26706177] |
| 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 | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526] |
| ChEMBL | Inhibition of [3H]GABA uptake at mouse GAT3 expressed in HEK cells | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300] |
| ChEMBL | Inhibition of GABA uptake at murine GAT-2 expressed in HEK293 cells | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Eur J Med Chem (2013) 65: 487-499 [PMID:23770450] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Eur J Med Chem (2014) 83: 256-273 [PMID:24973660] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting analysis | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Bioorg Med Chem (2019) 27: 144-152 [PMID:30503411] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK293 cells by [3H]GABA uptake assay | B | 5.3 | pIC50 | 5011.87 | nM | IC50 | Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617] |
| GAT3/GAT2 in Rat [GtoPdb: 931, 930] [UniProtKB: P31647, P31646] | ||||||||
| GtoPdb | - | - | 4.7 | pIC50 | 20000 | nM | IC50 | Recept Channels (1994) 2: 207-13 [PMID:7874447] |
| GAT3/GABA transporter 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3699] [GtoPdb: 931] [UniProtKB: P31650] | ||||||||
| ChEMBL | Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells | B | 4.66 | pIC50 | 22000 | nM | IC50 | Eur J Med Chem (2011) 46: 1483-1498 [PMID:21353350] |
| ChEMBL | Inhibition of mouse GAT3 mediated [3]GABA uptake expressed in HEK293 cells after 3 mins by scintillation counting | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 417-423 [PMID:26706177] |
| 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 | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2480-2488 [PMID:25882526] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| ChEMBL | Inhibition of mouse GAT3 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Eur J Med Chem (2021) 221: 113512-113512 [PMID:34015586] |
| ChEMBL | Inhibition of mouse GAT3 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition measured after 4 mins by liquid scintillation counting analysis | B | 5.29 | pIC50 | 5128.61 | nM | IC50 | Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK cells assessed as reduction in [3H]GABA uptake by measuring remaining [3H]GABA uptake levels preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting analysis | B | 5.65 | pIC50 | 2238.72 | nM | IC50 | Bioorg Med Chem (2019) 27: 144-152 [PMID:30503411] |
| ChEMBL | Inhibition of GABA uptake at murine GAT-3 expressed in HEK293 cells | B | 5.71 | pIC50 | 1949.84 | nM | IC50 | Eur J Med Chem (2013) 65: 487-499 [PMID:23770450] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK293 cells assessed as reduction in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition and measured after 4 mins by microbeta liquid scintillation counting method | B | 5.71 | pIC50 | 1949.84 | nM | IC50 | Bioorg Med Chem (2019) 27: 822-831 [PMID:30718063] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake preincubated for 25 mins followed by [3H]GABA addition measured after 4 mins by liquid scintillation counting analysis | B | 5.71 | pIC50 | 1949.84 | nM | IC50 | Bioorg Med Chem (2018) 26: 3668-3687 [PMID:29886082] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK293 cells assessed as decrease in [3H]GABA uptake | B | 5.71 | pIC50 | 1949.84 | nM | IC50 | Eur J Med Chem (2014) 83: 256-273 [PMID:24973660] |
| ChEMBL | Inhibition of mouse GAT4 expressed in human HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 40 mins by LC-ESI-MS/MS analysis | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | Eur J Med Chem (2021) 221: 113512-113512 [PMID:34015586] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK293 cells by [3H]GABA uptake assay | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | Bioorg Med Chem (2015) 23: 1284-1306 [PMID:25698617] |
| ChEMBL | Inhibition of mouse GAT4 expressed in HEK293 cell line assessed as inhibition of [3H]GABA uptake measured after 35 mins by liquid scintillation method | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | Eur J Med Chem (2020) 188: 111920-111920 [PMID:31901745] |
| ChEMBL | Inhibition of [3H]GABA uptake at mouse GAT4 expressed in HEK cells | B | 5.81 | pIC50 | 1548.82 | nM | IC50 | Eur J Med Chem (2008) 43: 2404-2411 [PMID:18395300] |
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]
