sabcomeline [Ligand Id: 306] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL134641 (Sabcomeline, SB-202026)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • 6.67
1 CHEMBL134641_lig_chart_1 Muscarinic acetylcholine receptor M1 Human
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 1 pki data point
  • 6.69
2 CHEMBL134641_lig_chart_2 Muscarinic acetylcholine receptor M2 Human
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
  • 7
3 CHEMBL134641_lig_chart_3 Muscarinic acetylcholine receptor M3 Human
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
  • 7.2
4 CHEMBL134641_lig_chart_4 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 1 pki data point
  • 7.1
5 CHEMBL134641_lig_chart_5 Muscarinic acetylcholine receptor M5 Human
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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 B 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 B 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 B 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 B 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 B 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 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]