PF-06767832 [Ligand Id: 9228] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4097569 |
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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 muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as accumulation of inositol phosphate measured after 30 mins by HTRF assay | F | 5.04 | pEC50 | >=9200 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| ChEMBL | Partial agonist activity at muscarinic M1 receptor (unknown origin) assessed as recruitment of beta-arrestin by Path Hunter assay | B | 5.41 | pEC50 | 3900 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| ChEMBL | Partial agonist activity at human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in intracellular calcium level measured after 10 mins by Fluo-8AM dye based FLIPR TETRA method | F | 5.41 | pEC50 | >=3900 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| ChEMBL | Positive allosteric modulation of muscarinic M1 receptor (unknown origin) expressed in CHO cells assessed as increase in Ach-induced accumulation of inositol phosphate accumulation measured after 30 mins by HTRF assay | F | 6.35 | pEC50 | 447 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| ChEMBL | Positive allosteric modulation of muscarinic M1 receptor (unknown origin) assessed as increase in Ach-induced recruitment of beta-arrestin by Path Hunter assay | B | 6.44 | pEC50 | 365 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| GtoPdb | FLIPR calcium mobilisation assay | - | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2016) 59: 6313-28 [PMID:27275946] |
| ChEMBL | Positive allosteric modulation of human muscarinic M1 receptor stably expressed in CHO cells assessed as increase in Ach-induced intracellular calcium level preincubated for 10 mins followed by addition of Ach at EC20 concentration by Fluo-8AM dye based FLIPR TETRA method | F | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9] | ||||||||
| ChEMBL | Inhibition of PDE11A4 (unknown origin) | B | 5.31 | pIC50 | 4940 | nM | IC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of PDE2A (unknown origin) | B | 5.51 | pIC50 | 3090 | nM | IC50 | J Med Chem (2016) 59: 6313-6328 [PMID:27275946] |
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]
