L-CCG-I [Ligand Id: 1368] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280563 (2S,1'S,2'S)-2-(Carboxycyclopropyl)Glycine) |
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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 | Inhibitory concentration against radioligand [3H]CGS-19,755 binding to N-methyl-D-aspartate glutamate receptor in rat forebrain membranes | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 528-537 [PMID:9046344] |
| 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 | Inhibitory concentration against radioligand [3H]AMPA binding to Ionotropic glutamate receptor AMPA in rat forebrain membranes | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 528-537 [PMID:9046344] |
| 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 | Inhibitory concentration against radioligand [3H]-Kainate binding to Ionotropic glutamate receptor kainate in rat forebrain membranes | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1997) 40: 528-537 [PMID:9046344] |
| 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 | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat | F | 4.64 | pEC50 | 23000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 2 agonist | F | 6.31 | pKi | 490 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in human | B | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - |
Br J Pharmacol (1998) 123: 497-504 [PMID:9504391]; Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat | B | 6.12 | pEC50 | 750 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Metabotropic glutamate receptor 2 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| 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 | 6.36 | pKi | 440 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - | Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.22 | pEC50 | 600 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| 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 | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | - | - | - | Br J Pharmacol (1992) 107: 539-43 [PMID:1330184] |
| ChEMBL | Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 5.4 | pEC50 | 4000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| 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 | 5.51 | pKi | 3100 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 5.8 | pIC50 | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Metabotropic glutamate receptor 5 agonist activity as basal [3H]- IP formation in rat | F | 4.77 | pEC50 | 17000 | 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 | 5.24 | pKi | 5800 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 6.2 | pEC50 | - | - | - | Neuropharmacology (1997) 36: 145-52 [PMID:9144651] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| GtoPdb | - | - | 5.2 | pEC50 | - | - | - | Neuropharmacology (1998) 37: 1043-51 [PMID:9833633] |
| ChEMBL | Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.22 | pEC50 | 600 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| GtoPdb | - | - | 4.3 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| ChEMBL | Metabotropic glutamate receptor 7 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells | F | 4.33 | pEC50 | 47000 | nM | EC50 | J Med Chem (2004) 47: 456-466 [PMID:14711315] |
| 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 | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 6.3 | pIC50 | - | - | - | Brain Res Mol Brain Res (1999) 67: 201-10 [PMID:10216218] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| GtoPdb | - | - | 6.2 | pEC50 | - | - | - | Mol Pharmacol (1997) 51: 119-25 [PMID:9016353] |
| ChEMBL | Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells | F | 6.4 | pEC50 | 400 | 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]
