ML375 [Ligand Id: 7631] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3105228 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 | Negative allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| ChEMBL | Antagonist activity at human muscarinic M1 receptor assessed as inhibition of acetylcholine-induced calcium response | F | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Negative allosteric modulation of rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Negative allosteric modulation of human muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| ChEMBL | Antagonist activity at human muscarinic M2 receptor assessed as inhibition of acetylcholine-induced calcium response | F | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Negative allosteric modulation of rat muscarinic acetylcholine receptor M2 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Negative allosteric modulation of human muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| ChEMBL | Antagonist activity at human muscarinic M3 receptor assessed as inhibition of acetylcholine-induced calcium response | F | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Negative allosteric modulation of rat muscarinic acetylcholine receptor M3 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Negative allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| ChEMBL | Antagonist activity at human muscarinic M4 receptor assessed as inhibition of acetylcholine-induced calcium response | F | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Negative allosteric modulation of rat muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay | F | 5.95 | pIC50 | 1110 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1356-1359 [PMID:28237763] |
| ChEMBL | Negative allosteric modulation of human M5 receptor expressed in CHO cells assessed as inhibition of acetyl choline-induced calcium mobilization preincubated for 150 secs followed by acetyl choline addition by Fluo-4-AM dye based fluorescence assay | F | 5.98 | pIC50 | 1047.13 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1356-1359 [PMID:28237763] |
| ChEMBL | Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
| ChEMBL | Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response | F | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4487-4491 [PMID:27503678] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
| ChEMBL | Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay | F | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2013) 56: 9351-9355 [PMID:24164599] |
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]
