VU0467154 [Ligand Id: 12301] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3915634 |
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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 | Displacement of [3H]-N-Methylscopolamine from human M1 receptor expressed in CHOK1 cells | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Binding affinity to rat M1 receptor by radio-ligand binding assay | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Displacement of [3H]-N-Methylscopolamine from human M2 receptor expressed in CHOK1 cells | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Binding affinity to rat M2 receptor by radio-ligand binding assay | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Displacement of [3H]-N-Methylscopolamine from human M3 receptor expressed in CHOK1 cells | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Binding affinity to rat M3 receptor by radio-ligand binding assay | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M4 receptor in Monkey [GtoPdb: 16] | ||||||||
| GtoPdb | - | - | 6 | pEC50 | 1000 | nM | EC50 | ACS Chem Neurosci (2014) 5: 920-42 [PMID:25137629] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay | F | 6.2 | pEC50 | 631 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| ChEMBL | Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay | F | 6.2 | pEC50 | 630.96 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| GtoPdb | Potentiation of ACh response at human receptor | - | 6.2 | pEC50 | 631 | nM | EC50 | ACS Chem Neurosci (2014) 5: 920-42 [PMID:25137629] |
| ChEMBL | Positive allosteric modulation of human M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mobilization | F | 7.04 | pEC50 | 91 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 5179-5184 [PMID:29089231] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| 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 | Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay | F | 7.75 | pEC50 | 17.8 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| GtoPdb | - | - | 7.75 | pEC50 | 17.8 | nM | EC50 | ACS Chem Neurosci (2014) 5: 920-42 [PMID:25137629] |
| ChEMBL | Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqui5 by calcium mobilization assay | F | 7.75 | pEC50 | 17.78 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to human M5 receptor by radio-ligand binding assay | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
| ChEMBL | Binding affinity to rat M5 receptor by radio-ligand binding assay | B | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 171-175 [PMID:27939174] |
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]
