PD 102807 [Ligand Id: 11498] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL59898 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.67 | pKi | 2157 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.3 | pKi | 500.15 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR3A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.78 | pKi | 1662.65 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.12 | pKi | 767 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA2B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.49 | pKi | 3225.15 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.23 | pKi | 585.19 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| FFA4 receptor/Free fatty acid receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | F | 5.88 | pEC50 | 1306.47 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35 | F | 5.39 | pIC50 | 4111.59 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.55 | pKi | 2836.94 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | PDSP Secondary Binding target: OPRK1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.71 | pKi | 1941.19 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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 | PDSP Secondary Binding target: CHRM3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.76 | pKi | 172.9 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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] | ||||||||
| ChEMBL | PDSP Secondary Binding target: CHRM4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 7.33 | pKi | 46.93 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 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] |
| μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | PDSP Secondary Binding target: OPRM1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.95 | pKi | 1130.71 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5.24 | pIC50 | 5760.74 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.17 | pKi | 673.28 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.55 | pKi | 2850.37 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
ChEMBL data shown on this page come from version 36:
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]
