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 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]
