(1S,3R)-ACPD [Ligand Id: 1365] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL34453 |
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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 | Affinity value against N-methyl-D-aspartate (NMDA) receptor using [3H]-CGS- 19755 in glutamate radioligand binding assay. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
| 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 | Affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA in selective radioligand binding assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
| 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 | Affinity value against Ionotropic glutamate receptor kainate using [3H]-kainic acid in selective radioligand binding assay. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1996) 39: 2990-3000 [PMID:8709133] |
| 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 | 4.38 | pKi | 42000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a) | B | 4.66 | pEC50 | 22000 | nM | EC50 | J Med Chem (1996) 39: 3998-4006 [PMID:8831765] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 1 | B | 4.82 | pEC50 | 15000 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| ChEMBL | Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation | F | 5.03 | pEC50 | 9300 | nM | EC50 | J Med Chem (1997) 40: 3119-3129 [PMID:9301676] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | - | - | - |
Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537]; Brain Res (1993) 619: 22-8 [PMID:7690672]; J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat | B | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 1 | F | 4.38 | pEC50 | 42000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR1a in rat | B | 4.66 | pEC50 | 22000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells | F | 4.82 | pEC50 | 15000 | nM | EC50 | J Med Chem (2003) 46: 3102-3108 [PMID:12825948] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| GtoPdb | - | - | 4.2 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2). | F | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Agonist activity against Metabotropic glutamate receptor 2 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation | F | 4.74 | pEC50 | 18000 | nM | EC50 | J Med Chem (1997) 40: 3119-3129 [PMID:9301676] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in human | B | 4.92 | pEC50 | 12100 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Compound was tested for the inhibition of metabotropic glutamate receptor 2 (mGluR2). | B | 5.7 | pEC50 | 2000 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| GtoPdb | - | - | 5.4 | 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 | 5.11 | pEC50 | 7700 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 2 | F | 5.3 | pEC50 | 5000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat | B | 5.3 | pEC50 | 5000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing mGluR2 receptor | F | 5.68 | pEC50 | 2100 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
| ChEMBL | Activity tested at cloned rat mGluR2 receptor expressed in Chinese Hamster Ovary (CHO) cells | F | 5.7 | pEC50 | 2000 | nM | EC50 | J Med Chem (2003) 46: 3102-3108 [PMID:12825948] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| GtoPdb | - | - | 4.7 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing chimeric mGluR3/1a receptor | F | 4.52 | pEC50 | 30000 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1721-1726 [PMID:10397508] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| GtoPdb | - | - | 4.8 | pKi | - | - | - | Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR3 in rat | B | 5.1 | pEC50 | 8000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 4.01 | pKi | 98000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | B | 4.41 | pEC50 | 39000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1447-1450 [PMID:10888329] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat | B | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2005) 48: 2534-2547 [PMID:15801843] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat | B | 4.41 | pEC50 | 39000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| 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 | 4.82 | pKi | 15000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 5 | B | 4.64 | pEC50 | 23000 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| GtoPdb | - | - | 5.7 | pIC50 | - | - | - | J Neurochem (2000) 75: 2590-601 [PMID:11080213] |
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR5a in rat | B | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| ChEMBL | Activity tested at cloned rat Metabotropic glutamate receptor 5 expressed in Chinese Hamster Ovary (CHO) cells | F | 4.64 | pEC50 | 23000 | nM | EC50 | J Med Chem (2003) 46: 3102-3108 [PMID:12825948] |
| ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 5 | F | 4.82 | pEC50 | 15000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
| 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 | 4.22 | pKi | 60000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Compound was tested for the inhibition of Metabotropic glutamate receptor 6 | B | 4.09 | pEC50 | 82000 | nM | EC50 | J Med Chem (1998) 41: 1641-1650 [PMID:9572889] |
| GtoPdb | - | - | 4.7 | 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 | - | - | 4.2 | pEC50 | - | - | - | Bioorg Med Chem Lett (1997) 7: 601-606 |
| ChEMBL | Tested for the agonistic activity against Metabotropic glutamate receptor 6 | F | 4.22 | pEC50 | 60000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 601-606 |
| 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 | 4.35 | pKi | 45000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 4.4 | pEC50 | - | - | - | Brain Res Mol Brain Res (1998) 53: 88-97 [PMID:9473604] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743] | ||||||||
| ChEMBL | Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse | B | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (1995) 38: 1417-1426 [PMID:7738999] |
| mGlu8 receptor in Rat [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| GtoPdb | - | - | 4.3 | pEC50 | - | - | - | Mol Pharmacol (1997) 51: 119-25 [PMID:9016353] |
| PLCβ1/Phospholipase C-beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4034] [GtoPdb: 1403] [UniProtKB: Q9NQ66] | ||||||||
| ChEMBL | Agonistic activity against phospholipase C (PLC) was determined in adult rat hippocampal slices | F | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (1999) 42: 2716-2720 [PMID:10411492] |
| mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| GtoPdb | - | - | 3 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
| GtoPdb | - | - | 3.1 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
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]
