sabcomeline [Ligand Id: 306] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL134641 (Sabcomeline, SB-202026, SKB-202026) |
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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 | 6.64 | pKi | 229.09 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594] |
| ChEMBL | In vitro affinity against human Muscarinic acetylcholine receptor M1 using quinuclidynyl benzylate (QNB) | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 7.2 | pEC50 | 63.6 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Binding affinity to human cloned muscarinic M2 receptor expressed in CHO cells | B | 6.69 | pKi | 204.17 | nM | Ki | Bioorg Med Chem (2008) 16: 3049-3058 [PMID:18182302] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M2 | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 7.21 | pEC50 | 62.1 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 7 | pKi | - | - | - | Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M3 | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.93 | pEC50 | 117 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | - | - | - | Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594] |
| ChEMBL | In vitro affinity is evaluated, using quinuclidynyl benzylate (QNB) as radioligand in human cloned Muscarinic acetylcholine receptor M4 | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (1997) 40: 4265-4280 [PMID:9435896] |
| ChEMBL | Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.67 | pEC50 | 214 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
| ChEMBL | Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay | F | 8.24 | pEC50 | 5.7 | nM | EC50 | ACS Med Chem Lett (2013) 4: 244-248 [PMID:24900656] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| GtoPdb | - | - | 7.1 | pKi | - | - | - | Br J Pharmacol (1999) 126: 1620-4 [PMID:10323594] |
| ChEMBL | Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay | F | 6.91 | pEC50 | 123 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 4158-4163 [PMID:26299349] |
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]
