VU0152100 [Ligand Id: 3263] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1978713
  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization B 6.17 pEC50 680 nM EC50 Bioorg Med Chem Lett (2019) 29: 362-366 [PMID:30580918]
ChEMBL Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay F 6.21 pEC50 620 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 346-350 [PMID:23177787]
ChEMBL Positive allosteric modulation of human M4 receptor B 6.28 pEC50 520 nM EC50 Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
GtoPdb - - 6.42 pEC50 380 nM EC50 J Pharmacol Exp Ther (2008) 327: 941-53 [PMID:18772318]
ChEMBL Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response B 6.64 pEC50 230 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 346-350 [PMID:23177787]
ChEMBL Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization F 6.65 pEC50 225 nM EC50 Bioorg Med Chem Lett (2017) 27: 4999-5001 [PMID:29037946]

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]