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 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]
