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 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]
