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ChEMBL ligand: CHEMBL43412 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 4.6 | pKi | 25000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
ChEMBL | Inhibitory activity against mGluR1 receptor | B | 4.49 | pIC50 | 32000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1569-1574 [PMID:9873392] |
ChEMBL | The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a | F | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (1996) 39: 2874-2876 [PMID:8709120] |
ChEMBL | Antagonist activity at mGlu1 receptor | F | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2007) 50: 2563-2568 [PMID:17489573] |
ChEMBL | Inhibition of mGluR1a receptor | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2011) 54: 2529-2591 [PMID:21413808] |
ChEMBL | Antagonist activity at mGluR1alpha (unknown origin) | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2021) 64: 14046-14128 [PMID:34591488] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
GtoPdb | - | - | 4.2 | pIC50 | 67000 | nM | IC50 | Neuropharmacology (1999) 38: 917-26 [PMID:10428410] |
ChEMBL | Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells. | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (1999) 42: 1546-1555 [PMID:10229625] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
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] |
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
GtoPdb | - | - | 4.3 | pEC50 | 47000 | nM | EC50 | Neuropharmacology (1999) 38: 917-26 [PMID:10428410] |
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]