muscarine [Ligand Id: 3996] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL12587 (L-(+)-muscarine, Muscarin) |
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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 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]
