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ChEMBL ligand: CHEMBL593590 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
ChEMBL | Displacement of radioligand from glutamate and glycine binding site of NMDA receptor in rat brain membrane | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
ChEMBL | Inhibition of human mGluR1 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
ChEMBL | Inhibition of human mGluR2 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
GtoPdb | - | - | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 184-8 [PMID:19931453] |
ChEMBL | Displacement of [3H]ABP688 from human recombinant mGluR5 expressed in CHO cells | B | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
ChEMBL | Antagonist activity at human mGluR5 assessed as inhibition of quisqualate-induced intracellular inositol phosphate accumulation | F | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
GtoPdb | - | - | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-8 [PMID:19931453] |
ChEMBL | Antagonist activity at human mGluR5 assessed as inhibition of glutamate-induced elevation of intracellular calcium concentration | F | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
ChEMBL | Displacement of [3H]ABP688 from mGluR5 in rat brain cortex | B | 7.52 | pKi | 30 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
ChEMBL | Inhibition of human mGluR7 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453] |
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]