LY307452 [Ligand Id: 3350] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL39338 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| ChEMBL | Binding affinity against Ionotropic glutamate receptor using [3H]-AMPA displacement from rat forebrain preparations | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 765-770 [PMID:9871538] |
| GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| ChEMBL | Binding affinity against Ionotropic glutamate receptor using [3H]-Kainate displacement from rat forebrain preparations | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 765-770 [PMID:9871538] |
| GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264] | ||||||||
| ChEMBL | Binding affinity against Ionotropic glutamate receptor using ACPD sensitive [3H]- glutamate displacement from rat forebrain preparations | B | 5.47 | pIC50 | 3380 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 765-770 [PMID:9871538] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Antagonist potency against cloned Metabotropic glutamate receptor 2 | F | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 2 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation | F | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 765-770 [PMID:9871538] |
| ChEMBL | In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 2 expressed in RGT cells. | F | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1985-1990 [PMID:9873471] |
| ChEMBL | Inhibitory activity against human Metabotropic glutamate receptor 2 | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1999) 42: 1546-1555 [PMID:10229625] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 4.52 | pKi | 30000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Tested for agonist activity in non-neuronal cells (RGT) expressing human Metabotropic glutamate receptor 3 by measuring ACPD (3 uM) induced inhibition of forskolin (15 uM)-stimulated cAMP formation | F | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 765-770 [PMID:9871538] |
| ChEMBL | In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells. | F | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1985-1990 [PMID:9873471] |
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]
