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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
