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ChEMBL ligand: CHEMBL59898 (PD-102807) |
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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 | 5.84 | pKi | 1430 | 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 | 5.99 | pKi | 1030 | 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 | Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor expressed in CHO-K1 cells | B | 5.64 | pKi | 2290.87 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M1 in transfected CHO cells. | B | 5.88 | pKi | 1318.26 | nM | Ki | J Med Chem (2002) 45: 3094-3102 [PMID:12086495] |
ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m1 by displacement of [3H]NMS binding using membranes in transfected chinese hamster ovarian cell | B | 5.18 | pIC50 | 6558.7 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M2 receptor expressed in CHO-K1 cells | B | 5.96 | pKi | 1096.48 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Inhibition of [3H]-NMS binding to human muscarinic acetylcholine receptor M2 in transfected CHO cells. | B | 6.27 | pKi | 537.03 | nM | Ki | J Med Chem (2002) 45: 3094-3102 [PMID:12086495] |
ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m2 by displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 5.46 | pIC50 | 3440.7 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cells | B | 6.14 | pKi | 724.44 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells. | B | 6.59 | pKi | 257.04 | nM | Ki | J Med Chem (2002) 45: 3094-3102 [PMID:12086495] |
ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m3 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 6.02 | pIC50 | 950 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
GtoPdb | - | - | 7.6 | pKi | - | - | - |
Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897]; Life Sci (1999) 65: 2233-40 [PMID:10576595] |
ChEMBL | Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells. | B | 8.15 | pKi | 7.08 | nM | Ki | J Med Chem (2002) 45: 3094-3102 [PMID:12086495] |
ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO-K1 cells | B | 8.19 | pKi | 6.46 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation | F | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m4 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 7.04 | pIC50 | 90.7 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
ChEMBL | Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as blockade of carbachol-induced inhibition of forskolin-stimulated cAMP accumulation | F | 7.27 | pEC50 | 54 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M5 in transfected CHO cells. | B | 5.47 | pKi | 3388.44 | nM | Ki | J Med Chem (2002) 45: 3094-3102 [PMID:12086495] |
ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO-K1 cells | B | 5.74 | pKi | 1819.7 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2972-2976 [PMID:18395442] |
ChEMBL | Evaluated for its binding affinity at human muscarinic receptor m5 by the displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell | B | 5.13 | pIC50 | 7411.7 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1991-1996 [PMID:9873472] |
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]