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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
