(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 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]
