VU0238429 [Ligand Id: 3257] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL466253 (VU0238429)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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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]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Rat [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
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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 Positive allosteric modulation of human muscarinic M1 receptor B 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization B 4.52 pEC50 >30000 nM EC50 J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Positive allosteric modulation of human muscarinic M2 receptor B 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization F 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 558-562 [PMID:20004578]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization B 4.52 pEC50 >30000 nM EC50 J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
ChEMBL Positive allosteric modulation of human muscarinic M3 receptor B 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Positive allosteric modulation of human muscarinic M4 receptor B 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization F 4.52 pEC50 >30000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 558-562 [PMID:20004578]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein by scintillation counting B 5.79 pKi 1610 nM Ki J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
ChEMBL Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein by scintillation counting in presence of acetylcholine B 6.8 pKi 159 nM Ki J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
ChEMBL Positive allosteric modulation activity at muscarinic M5 receptor B 5.92 pEC50 1200 nM EC50 J. Med. Chem. (2012) 55: 1445-1464 [PMID:22148748]
ChEMBL Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization B 5.94 pEC50 1160 nM EC50 J. Med. Chem. (2009) 52: 3445-3448 [PMID:19438238]
GtoPdb - - 5.94 pEC50 1160 nM EC50 J Med Chem (2009) 52: 3445-8 [PMID:19438238]
ChEMBL Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization F 5.96 pEC50 1100 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 558-562 [PMID:20004578]
ChEMBL Positive allosteric modulation of human muscarinic M5 receptor B 5.96 pEC50 1100 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
ChEMBL Positive allosteric modulation of rat muscarinic M5 receptor B 8.34 pEC50 4.58 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
ChEMBL Positive allosteric modulation of rat muscarinic M5 receptor B 8.34 pEC50 4.57 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
ChEMBL Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response B 9.58 pEC50 0.26 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]
ChEMBL Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response B 9.58 pEC50 0.26 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 2996-3000 [PMID:23562060]

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]