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 B 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 B 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]