arecaidine propargyl ester [Ligand Id: 295] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL128365 (Arecaidine Propargyl Ester)
  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
ChEMBL Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting B 5.28 pKi 5200 nM Ki J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687]
ChEMBL Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting B 5.35 pKi 4490 nM Ki J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to cloned human muscarinic M1 receptor expressed in CHO cells B 5.91 pKi 1230.27 nM Ki J Med Chem (2006) 49: 1925-1931 [PMID:16539379]
GtoPdb - - 6.4 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
GtoPdb - - 5.7 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Binding affinity to cloned human muscarinic M2 receptor expressed in CHO cells B 7.06 pKi 87.1 nM Ki J Med Chem (2006) 49: 1925-1931 [PMID:16539379]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
GtoPdb - - 5.7 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Binding affinity to cloned human muscarinic M3 receptor expressed in CHO cells B 6.07 pKi 851.14 nM Ki J Med Chem (2006) 49: 1925-1931 [PMID:16539379]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 5.9 pKi - - - Mol Pharmacol (1997) 52: 172-9 [PMID:9224827]
ChEMBL Binding affinity to cloned human muscarinic M4 receptor expressed in CHO cells B 6.01 pKi 977.24 nM Ki J Med Chem (2006) 49: 1925-1931 [PMID:16539379]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Binding affinity to cloned human muscarinic M5 receptor expressed in CHO cells B 6.03 pKi 933.25 nM Ki J Med Chem (2006) 49: 1925-1931 [PMID:16539379]

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]