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 F 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 F 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 F 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 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]