ML375 [Ligand Id: 7631] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3105228
  • 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]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
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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 Negative allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
ChEMBL Antagonist activity at human muscarinic M1 receptor assessed as inhibition of acetylcholine-induced calcium response B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
ChEMBL Negative allosteric modulation of rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Negative allosteric modulation of human muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
ChEMBL Antagonist activity at human muscarinic M2 receptor assessed as inhibition of acetylcholine-induced calcium response B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678]
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
ChEMBL Negative allosteric modulation of rat muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Negative allosteric modulation of human muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
ChEMBL Antagonist activity at human muscarinic M3 receptor assessed as inhibition of acetylcholine-induced calcium response B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678]
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
ChEMBL Negative allosteric modulation of rat muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Negative allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
ChEMBL Antagonist activity at human muscarinic M4 receptor assessed as inhibition of acetylcholine-induced calcium response B 4.52 pIC50 >30000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678]
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
ChEMBL Negative allosteric modulation of rat muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay B 5.95 pIC50 1110 nM IC50 Bioorg Med Chem Lett (2017) 27: 1356-1359 [PMID:28237763]
ChEMBL Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay B 5.98 pIC50 1047.13 nM IC50 Bioorg Med Chem Lett (2017) 27: 1356-1359 [PMID:28237763]
ChEMBL Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 6.52 pIC50 300 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]
ChEMBL Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response B 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678]
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
ChEMBL Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay F 6.1 pIC50 790 nM IC50 J. Med. Chem. (2013) 56: 9351-9355 [PMID:24164599]

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]