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ChEMBL ligand: CHEMBL17045 (AF-DX 116, AF-DX-116, Otenzepad) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 5.86 | pKi | 1380 | 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 | 5.91 | pKi | 1220 | 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 | - | - | 6.2 | pKd | - | - | - | Biochem Pharmacol (1996) 52: 643-58 [PMID:8759038] |
ChEMBL | Binding affinity to human M1 muscarinic receptor | B | 6.27 | pKi | 537 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
ChEMBL | Compound was evaluated for displacement of [3H]QNB from human Muscarinic m1 receptor in CHO cells. | B | 6.75 | pKi | 179 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
M1 receptor in Rat [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
GtoPdb | - | - | 6.3 | pKi | - | - | - |
Life Sci (1992) 51: 955-71 [PMID:1325587]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Binding affinity to human M2 muscarinic receptor | B | 7.09 | pKi | 81 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
GtoPdb | - | - | 7.2 | pKi | - | - | - |
Mol Pharmacol (1989) 35: 469-76 [PMID:2704370]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790] |
ChEMBL | Compound was evaluated for displacement of [3H]-QNB from human Muscarinic m2 receptor in CHO cells. | B | 7.28 | pKi | 52 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 785-788 |
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
GtoPdb | - | - | 7.3 | pKi | - | - | - |
EMBO J (1988) 7: 3031-5 [PMID:2846274]; Life Sci (1992) 51: 955-71 [PMID:1325587]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790] |
ChEMBL | Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Inhibition of muscarinic (M2) receptor isolated from rat atria | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
ChEMBL | Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Inhibition of muscarinic (M2) receptor isolated from rat atria | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
ChEMBL | Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Inhibition of muscarinic (M2) receptor isolated from rat atria | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Binding affinity to human M3 muscarinic receptor | B | 5.68 | pKi | 2089 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
GtoPdb | - | - | 6.1 | pKi | - | - | - | Mol Pharmacol (1989) 35: 469-76 [PMID:2704370] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
GtoPdb | - | - | 6 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
ChEMBL | Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
ChEMBL | Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1989) 32: 1718-1724 [PMID:2754696] |
ChEMBL | Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
ChEMBL | Inhibition of rat submandibular muscarinic (M3) receptor isolated from tissue homogenates | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (1994) 37: 3775-3788 [PMID:7966137] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
GtoPdb | - | - | 7 | pKd | - | - | - | Biochem Pharmacol (1996) 52: 643-58 [PMID:8759038] |
ChEMBL | Binding affinity to human M4 muscarinic receptor | B | 6.39 | pKi | 407 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
M4 receptor in Rat [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
GtoPdb | - | - | 6.5 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
GtoPdb | - | - | 5.6 | pKi | - | - | - | Mol Pharmacol (1989) 35: 469-76 [PMID:2704370] |
M5 receptor in Rat [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
GtoPdb | - | - | 5.7 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
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]