PD 102807 [Ligand Id: 11498] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL59898 (PD-102807)
  • Muscarinic acetylcholine receptor DM1 in Drosophila melanogaster [ChEMBL: CHEMBL2366467] [UniProtKB: P16395]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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 5.84 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 31:

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]