emraclidine [Ligand Id: 13626] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5314557 (Cvl-231, CVL-231, Emraclidine, Pf-06852231, PF-06852231) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Agonist activity at human M1 receptor | F | 4.88 | pEC50 | >13300 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human M1 receptor | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Antagonist activity at human M1 receptor | F | 5.12 | pEC50 | >7500 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antagonist activity at human M2 receptor | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human muscarinic M2 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay | F | 5.24 | pEC50 | 5700 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Agonist activity at human M2 receptor | F | 5.29 | pEC50 | 5140 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human M2 receptor | B | 5.32 | pEC50 | 4798 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Agonist activity at human M3 receptor | F | 4.88 | pEC50 | >13300 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human M3 receptor | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Antagonist activity at human M3 receptor | F | 5.12 | pEC50 | >7500 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Antagonist activity at human M4 receptor | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Agonist activity at human M4 receptor | F | 7.05 | pEC50 | 89.5 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| GtoPdb | Determined in human M4 HEK293 cell assay using EC20 of acetylcholine. | - | 7.91 | pEC50 | 12.2 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay | F | 7.91 | pEC50 | 12.2 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Positive allosteric modulation of rat muscarinic M4 receptor expressed in HEK293 cells in presence of EC20 concentration of acetylcholine by Glosensor cAMP assay | F | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Agonist activity at human M5 receptor | F | 4.88 | pEC50 | >13300 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Positive allosteric modulation of human M5 receptor | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
| ChEMBL | Antagonist activity at human M5 receptor | F | 5.12 | pEC50 | >7500 | nM | EC50 | J Med Chem (2024) 67: 10831-10847 [PMID:38888621] |
ChEMBL data shown on this page come from version 36:
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]
