FITM [Ligand Id: 8767] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL566581 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
| ChEMBL | Displacement of [3H]quisqualate from human mGluR1 quisqualic acid binding site | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5464-5468 [PMID:19674894] |
| ChEMBL | Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay | F | 8.29 | pIC50 | 5.1 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5464-5468 [PMID:19674894] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| ChEMBL | Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (2012) 55: 2342-2352 [PMID:22316010] |
| GtoPdb | Measured using rat brain homogenate in a competition binding assay displacing [18F}-FITM. | - | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (2012) 55: 2342-52 [PMID:22316010] |
| ChEMBL | Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr | B | 7.86 | pIC50 | 13.9 | nM | IC50 | J Med Chem (2012) 55: 2342-2352 [PMID:22316010] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Inhibition of human mGluR2 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5464-5468 [PMID:19674894] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Antagonist activity at human mGluR5 receptor expressed in CHO cells by FLIPR assay | F | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5464-5468 [PMID:19674894] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Displacement of [11C]-ABP688 from mGluR5 in Sprague-Dawley rat brain homogenates after 1 hr by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 2342-2352 [PMID:22316010] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Inhibition of human mGluR8 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5464-5468 [PMID:19674894] |
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]
