VU0119498 [Ligand Id: 7632] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL523685 (VU0119498)
  • 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]
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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]
GtoPdb - - 5.2 pEC50 6040 nM EC50 J Med Chem (2009) 52: 3445-8 [PMID:19438238]
ChEMBL Positive allosteric modulation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay F 5.21 pEC50 6100 nM EC50 Bioorg Med Chem Lett (2010) 20: 5617-5622 [PMID:20801651]
ChEMBL Positive allosteric modulation activity at muscarinic M1 receptor B 5.22 pEC50 6000 nM EC50 J Med Chem (2012) 55: 1445-1464 [PMID:22148748]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization F 5.21 pEC50 6100 nM EC50 Bioorg Med Chem Lett (2010) 20: 558-562 [PMID:20004578]
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 5.22 pEC50 6040 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 muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay F 4.52 pEC50 >30000 nM EC50 Bioorg Med Chem Lett (2010) 20: 5617-5622 [PMID:20801651]
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 Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization F 5.19 pEC50 6400 nM EC50 Bioorg Med Chem Lett (2010) 20: 558-562 [PMID:20004578]
ChEMBL Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay F 5.19 pEC50 6400 nM EC50 Bioorg Med Chem Lett (2010) 20: 5617-5622 [PMID:20801651]
ChEMBL Positive allosteric modulation activity at muscarinic M3 receptor B 5.19 pEC50 6400 nM EC50 J Med Chem (2012) 55: 1445-1464 [PMID:22148748]
ChEMBL Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization F 5.2 pEC50 6380 nM EC50 J Med Chem (2009) 52: 3445-3448 [PMID:19438238]
GtoPdb - - 5.2 pEC50 6380 nM EC50 J Med Chem (2009) 52: 3445-8 [PMID:19438238]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Positive allosteric modulation of muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay F 4.52 pEC50 >30000 nM EC50 Bioorg Med Chem Lett (2010) 20: 5617-5622 [PMID:20801651]
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 Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay F 5.34 pEC50 4600 nM EC50 Bioorg Med Chem Lett (2010) 20: 5617-5622 [PMID:20801651]
ChEMBL Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization F 5.39 pEC50 4100 nM EC50 Bioorg Med Chem Lett (2010) 20: 558-562 [PMID:20004578]
ChEMBL Positive allosteric modulation activity at muscarinic M5 receptor B 5.39 pEC50 4100 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 5.39 pEC50 4080 nM EC50 J Med Chem (2009) 52: 3445-3448 [PMID:19438238]
GtoPdb - - 5.4 pEC50 4080 nM EC50 J Med Chem (2009) 52: 3445-8 [PMID:19438238]

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]