AFDX384 [Ligand Id: 3264] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL279453 (AF-DX-384) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366467] [UniProtKB: P16395] | ||||||||
| ChEMBL | Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting | B | 8.21 | pKi | 6.1 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| ChEMBL | Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting | B | 8.32 | pKi | 4.8 | nM | Ki | J Agric Food Chem (2007) 55: 2276-2281 [PMID:17319687] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - | J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M1 expressed in CHO cells by [3H]NMS displacement. | B | 7.51 | pKi | 30.9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M1 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.51 | pKi | 30.9 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Compound was evaluated for displacement of [3H]QNB from human Muscarinic m1 receptor in CHO cells. | B | 7.91 | pKi | 12.4 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement. | B | 8.22 | pKi | 6.03 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8.22 | pKi | 6.03 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Compound was evaluated for displacement of [3H]-QNB from human Muscarinic m2 receptor in CHO cells. | B | 8.28 | pKi | 5.28 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement. | B | 7.18 | pKi | 66.07 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M3 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 7.18 | pKi | 66.07 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 7.2 | pKi | - | - | - | J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - |
J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement. | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M4 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Affinity for Muscarinic acetylcholine receptor M5 expressed in CHO cells by [3H]NMS displacement. | B | 6.27 | pKi | 537.03 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1241-1243 [PMID:11354386] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M5 receptor expressed in stable CHO-K1 cells by radioligand binding assay | B | 6.27 | pKi | 537.03 | nM | Ki | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| GtoPdb | - | - | 6.3 | pKi | - | - | - | J Pharmacol Exp Ther (1991) 256: 727-33 [PMID:1994002] |
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]
