ML375 [Ligand Id: 7631] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3105228 |
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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 | 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 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]
