muscarine [Ligand Id: 3996] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12587 (L-(+)-muscarine, Muscarin)
  • 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 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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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 human cloned muscarinic M1 receptor expressed in CHO cells B 4.74 pKi 18197.01 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M1 expressed in CHO cell membranes B 7.25 pKi 56 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Tested for muscarinic binding affinity (Kapp) with 1 nM [3H]pirenzepine in rat cortex B 4.55 pKd 28 uM K app J. Med. Chem. (1987) 30: 969-975 [PMID:3585909]
ChEMBL In vitro 100 nM cortex affinity to displace [3H]- -pirenzepine providing a measure of muscarinic m1 receptor antagonist affinity F 5.25 pKi 5680 nM Ki Bioorg. Med. Chem. Lett. (1992) 2: 815-820
ChEMBL Inhibition of binding of [3H]oxotremorine M to Muscarinic acetylcholine receptor M1 in rat cerebral cortical membranes B 7.57 pKi 27 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Affinity versus [3H]oxotremorine M (agonist) binding to Muscarinic acetylcholine receptor M1 in Rat Cerebral Cortical Membranes, (Kd=0.75 nM) B 7.57 pKi 27 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL In vitro 100 nM cortex affinity to displace [3H]- -CD providing a measure of muscarinic m1 receptor agonist affinity F 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (1992) 2: 815-820
ChEMBL Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue. B 5.25 pIC50 5680 nM IC50 J. Med. Chem. (1992) 35: 15-27 [PMID:1732522]
ChEMBL Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M1 F 6.66 pEC50 219 nM EC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Dissociation constant at muscarinic acetylcholine receptor M2 of guinea pig heart(atria rate). B 4.61 pKd 4.61 - -Log KD J. Med. Chem. (1992) 35: 3102-3110 [PMID:1507199]
ChEMBL Dissociation constant at muscarinic acetylcholine receptor M2 guinea pig heart(atria force). B 4.7 pKd 4.7 - -Log KD J. Med. Chem. (1992) 35: 3102-3110 [PMID:1507199]
ChEMBL Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells B 6.31 pKi 489.78 nM Ki Bioorg. Med. Chem. (2008) 16: 3049-3058 [PMID:18182302]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M2 B 7.12 pKi 75 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membranes B 7.14 pKi 72 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membrane B 7.6 pKi 25 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the presence of GTP B 5.41 pIC50 3900 nM IC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the absence of GTP B 6.35 pIC50 449 nM IC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Tested for muscarinic binding affinity (Kapp) with 0.2 nM [3H]N-methylscopolamine in rat heart B 5.64 pKd 2.3 uM K app J. Med. Chem. (1987) 30: 969-975 [PMID:3585909]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes B 7.12 pKi 75 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibition of binding of 0.1 nM [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes of transfected CHO cells in the presence of 10 uM GTP B 5.41 pIC50 3900 nM IC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibition of binding of 0.1 nM [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes of transfected CHO cells in the absence of GTP B 6.31 pIC50 490 nM IC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL Inhibitory activity against stimulation of [3H]inositol monophosphate accumulation in [3H]inositol-labelled CHO transfected cells mediated by Muscarinic acetylcholine receptor M3 F 6.89 pEC50 130 nM EC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
ChEMBL Dissociation constant at muscarinic acetylcholine receptor M3 guinea pig bladder. B 4.62 pKd 4.62 - -Log KD J. Med. Chem. (1992) 35: 3102-3110 [PMID:1507199]
ChEMBL Dissociation constant at muscarinic acetylcholine receptor M3 of guinea pig ileum. B 5.95 pKd 5.95 - -Log KD J. Med. Chem. (1992) 35: 3102-3110 [PMID:1507199]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to muscarinic receptors in membranes of CHO cells transfected with Muscarinic acetylcholine receptor M3 B 4.55 pKi 28000 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes B 5.85 pKi 1400 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
ChEMBL Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes B 7.64 pKi 23 nM Ki J. Med. Chem. (2000) 43: 2514-2522 [PMID:10891110]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes B 5.85 pKi 1400 nM Ki J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]
ChEMBL Inhibitory activity against [3H]-cyclic AMP accumulation in CHO transfected cells mediated by Muscarinic acetylcholine receptor M4 F 6.33 pIC50 470 nM IC50 J. Med. Chem. (1998) 41: 2047-2055 [PMID:9622546]

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]