[3H]AF DX-384 [Ligand Id: 368] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL279453 (AF-DX-384)
  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
  • 8.27
1 CHEMBL279453_lig_chart_1 Muscarinic acetylcholine receptor DM1 Drosophila melanogaster
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • 7.51
2 CHEMBL279453_lig_chart_2 Muscarinic acetylcholine receptor M1 Human
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • 8.22
3 CHEMBL279453_lig_chart_3 Muscarinic acetylcholine receptor M2 Human
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • 7.18
4 CHEMBL279453_lig_chart_4 Muscarinic acetylcholine receptor M3 Human
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 8
5 CHEMBL279453_lig_chart_5 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 6.27
6 CHEMBL279453_lig_chart_6 Muscarinic acetylcholine receptor M5 Human
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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]
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 - - 9 pKd - - - J Pharmacol Exp Ther (1991) 259: 601-7 [PMID:1941609];
Front Pharmacol (2018) 9: 124 [PMID:29515448];
Brain Sci (2020) 10: [PMID:32079174]
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]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 8.7 pKd - - - J Pharmacol Exp Ther (1991) 259: 601-7 [PMID:1941609];
Front Pharmacol (2018) 9: 124 [PMID:29515448];
Brain Sci (2020) 10: [PMID:32079174]
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]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]