AQ-RA 741 [Ligand Id: 8584] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL43383
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]