LY379268 [Ligand Id: 1394] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275079 (LY-379268) |
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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 | Ability to displace [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| 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 | Ability to displace [3H]-KA binding to Ionotropic glutamate receptor kainate from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]-KA binding to Ionotropic glutamate receptor kainate from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]-KA binding to Ionotropic glutamate receptor kainate from rat forebrain | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
| ChEMBL | Agonist potency against cloned human metabotropic glutamate receptor 1 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR1a | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 2 subtypes expressed in RGT cells. | B | 5.7 | pKi | 2000 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 2 subtypes expressed in RGT cells. | B | 7.44 | pKi | 36.5 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 2 subtypes expressed in RGT cells. | B | 7.85 | pKi | 14.1 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Displacement of [3H]LY341495 from human recombinant mGluR2 in RGT cells | B | 7.85 | pKi | 14.1 | nM | Ki | J Med Chem (2007) 50: 233-240 [PMID:17228865] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | J Med Chem (1999) 42: 1027-40 [PMID:10090786] |
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2). | F | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Agonist activity at human mGluR2 assessed as effect on cAMP production in RGT cells | F | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2007) 50: 233-240 [PMID:17228865] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 2 | F | 8.57 | pEC50 | 2.69 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Agonist activity at human mGLUR2 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assay | F | 8.57 | pEC50 | 2.69 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| GtoPdb | - | - | 4.8 | pKi | - | - | - | J Med Chem (1999) 42: 1027-40 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells. | B | 5.98 | pKi | 1040 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells. | B | 7.84 | pKi | 14.3 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells. | B | 8.24 | pKi | 5.8 | nM | Ki | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells | B | 8.24 | pKi | 5.8 | nM | Ki | J Med Chem (2007) 50: 233-240 [PMID:17228865] |
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells | F | 8.34 | pEC50 | 4.6 | nM | EC50 | J Med Chem (2007) 50: 233-240 [PMID:17228865] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3 | F | 8.34 | pEC50 | 4.58 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Agonist activity at human mGLUR3 assessed as inhibition of forskolin-stimulated cAMP production by cell-based assay | F | 8.34 | pEC50 | 4.58 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) | F | 4.68 | pKi | 21000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a | F | 4.68 | pEC50 | 21100 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Agonist potency against cloned metabotropic glutamate receptor 5 | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6). | F | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 6.4 | pIC50 | - | - | - | J Med Chem (1999) 42: 1027-40 [PMID:10090786] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR5a | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6 | F | 6.4 | pEC50 | 401 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7). | F | 4 | pKi | >100000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR7 | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | F | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8 | F | 5.77 | pEC50 | 1690 | nM | EC50 | J Med Chem (1999) 42: 1027-1040 [PMID:10090786] |
| ChEMBL | Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells | F | 5.77 | pEC50 | 1690 | nM | EC50 | J Med Chem (2007) 50: 233-240 [PMID:17228865] |
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]
