otenzepad [Ligand Id: 309] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
