VU0152100 [Ligand Id: 3263] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1978713 |
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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 | F | 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] |
| ChEMBL | Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay | F | 6.31 | pEC50 | 495 | nM | EC50 | Bioorg Med Chem Lett (2021) 53: 128416-128416 [PMID:34710625] |
| 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 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]
