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