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 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]
