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ChEMBL ligand: CHEMBL466253 (VU0238429) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]