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 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]
