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 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]
