(R,S)-4-PPG [Ligand Id: 1406] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL277475 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat brain membrane | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1992) 35: 1345-1370 [PMID:1533422] |
| 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 | 5.28 | pKi | 5200 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | F | 5.28 | pEC50 | 5200 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
| GtoPdb | - | - | 5.3 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390] |
| ChEMBL | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | B | 5.33 | pEC50 | 4700 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1447-1450 [PMID:10888329] |
| ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR4a | F | 5.49 | pEC50 | 3200 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.28 | pEC50 | 5200 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| 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 | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 5.3 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| ChEMBL | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.33 | pEC50 | 4700 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| GtoPdb | - | - | 3.7 | pIC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390] |
| ChEMBL | Compound was evaluated for the inhibition of forskolin stimulated cAMP accumulation in CHO cells expressing hmGluR7b | F | 4.32 | pEC50 | 48000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1241-1244 [PMID:10866390] |
| 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 | 6.68 | pKi | 210 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 6.7 | pEC50 | - | - | - |
J Pharmacol Exp Ther (1999) 289: 1678-1687 [PMID:10336568]; Bioorg Med Chem Lett (2000) 10: 1241-4 [PMID:10866390]; Neuropharmacology (2001) 40: 311-8 [PMID:11166323] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| ChEMBL | Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.68 | pEC50 | 210 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
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]
