AQ-RA 741 [Ligand Id: 8584] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL43383 |
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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 | Binding affinity to muscarinic M1 receptor (unknown origin) expressed in CHO cells | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M1 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.54 | pKi | 28.84 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Tested for affinity constant against M1 muscarinic receptor in rat cortex using [3H]pirenzepine | B | 6.98 | pKi | 104.71 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Affinity constant measured against M1 muscarinic receptor in rat cortex | B | 7.6 | pKi | 25.12 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist] | F | 8.03 | pKd | 9.33 | nM | Kd | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Antagonistic activity measured in isolated guinea pig left atrium (M2 receptor) | F | 8.5 | pKd | 3.16 | nM | Kd | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Binding affinity to muscarinic M2 receptor (unknown origin) expressed in CHO cells | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8.37 | pKi | 4.27 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Affinity constant measured against M2 muscarinic receptor in rat heart | B | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Tested for affinity constant against M2 muscarinic receptor rat heart using [3H]-NMS | B | 8.49 | pKi | 3.24 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Binding affinity to muscarinic M3 receptor (unknown origin) expressed in CHO cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 7.3 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS | B | 6.6 | pKi | 251.19 | nM | Ki | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| ChEMBL | Affinity constant measured against M3 muscarinic receptor in rat submaxillary gland | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26] | ||||||||
| ChEMBL | Antagonistic activity measured in isolated guinea pig left ileum (M3 receptor) | F | 6.6 | pKd | 251.19 | nM | Kd | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| ChEMBL | Antagonistic activity against M3 muscarinic receptor in guinea pig left ileum derived by plotting log(DR - 1) vs log[antagonist] | F | 7 | pKd | 100 | nM | Kd | J Med Chem (1994) 37: 3363-3372 [PMID:7932564] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Binding affinity to muscarinic M4 receptor (unknown origin) expressed in CHO cells | B | 8.1 | pKi | 7.94 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8.19 | pKi | 6.46 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Affinity constant measured against M4 muscarinic receptor rat NG108-15 cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1993) 36: 3734-3737 [PMID:8246244] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to muscarinic M5 receptor (unknown origin) expressed in CHO cells | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M5 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 6.08 | pKi | 831.76 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
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]
