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 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]
