oxybutynin [Ligand Id: 359] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1231 (Anturol, Contimin 2.5, Contimin 5, Cystrin, Ditropan, Ditropan xl, Kentera, Lyrinel xl, Oxybutynin, Oxytrol, Oxytrol for women, Promictuline, Urimin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6.22 | pIC50 | 600 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.84 | pKi | 145.6 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 6.37 | pIC50 | 428.8 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 7.17 | pKi | 67.9 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 7.07 | pIC50 | 85.5 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Lethal(3)malignant brain tumor-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468] | ||||||||
| ChEMBL | Inhibition of L3MBTL1 by alpha-screening | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 7625-7631 [PMID:20931980] |
| L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7] | ||||||||
| ChEMBL | Inhibition of L3MBTL3 by alpha-screening | B | 4.27 | pIC50 | >54000 | nM | IC50 | J Med Chem (2010) 53: 7625-7631 [PMID:20931980] |
| Lethal(3)malignant brain tumor-like protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19] | ||||||||
| ChEMBL | Inhibition of L3MBTL4 by alpha-screening | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 7625-7631 [PMID:20931980] |
| MBT domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287625] [UniProtKB: Q05BQ5] | ||||||||
| ChEMBL | Inhibition of MBTD1 by alpha-screening | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2010) 53: 7625-7631 [PMID:20931980] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| GtoPdb | - | - | 8.6 | pKi | 2.4 | nM | Ki |
J Med Chem (2012) 55: 1783-7 [PMID:22243489]; Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605] |
| ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor expressed in CHO cells after 120 mins by scintillation counting | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (2012) 55: 1783-1787 [PMID:22243489] |
| ChEMBL | Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M1 receptor expressed in Sf9 cells | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 925-931 [PMID:17188867] |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.07 | pKi | 0.85 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.45 | pIC50 | 3.52 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| GtoPdb | - | - | 8.2 | pKi | - | - | - | J Med Chem (2005) 48: 6597-606 [PMID:16220976] |
| ChEMBL | Binding affinity for rat cortex muscarinic acetylcholine receptor M1 using [3H]pirenzepine | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2005) 48: 6597-6606 [PMID:16220976] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antagonism at muscarinic M2 receptor in isolated guinea pig urinary bladder | F | 7.4 | pKd | 39.81 | nM | Kd | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| ChEMBL | Binding affinity to human muscarinic M2 receptor | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M2 receptor expressed in CHO cells after 120 mins by scintillation counting | B | 7.93 | pKi | 11.75 | nM | Ki | J Med Chem (2012) 55: 1783-1787 [PMID:22243489] |
| GtoPdb | - | - | 7.93 | pKi | 11.75 | nM | Ki | J Med Chem (2012) 55: 1783-7 [PMID:22243489] |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.02 | pKi | 9.61 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M2 receptor expressed in Sf9 cells | B | 8.09 | pKi | 8.1 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 925-931 [PMID:17188867] |
| GtoPdb | - | - | 8.1 | pKi | - | - | - |
J Med Chem (2012) 55: 1783-7 [PMID:22243489]; Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605] |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 7.57 | pIC50 | 27 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Binding affinity for rat heart muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 6597-6606 [PMID:16220976] |
| ChEMBL | Affinity for rat Muscarinic acetylcholine receptor M2 | B | 8.16 | pKi | 6.97 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2093-2096 [PMID:15808475] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | - | - | - |
J Med Chem (2012) 55: 1783-7 [PMID:22243489]; Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605] |
| ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in CHO cells after 120 mins by scintillation counting | B | 8.82 | pKi | 1.51 | nM | Ki | J Med Chem (2012) 55: 1783-1787 [PMID:22243489] |
| ChEMBL | Binding affinity to human muscarinic M3 receptor | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| ChEMBL | Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells | B | 9.11 | pKi | 0.78 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 925-931 [PMID:17188867] |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.24 | pKi | 0.57 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.57 | pIC50 | 2.71 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine | B | 8.28 | pKi | 5.3 | nM | Ki | J Med Chem (2005) 48: 6597-6606 [PMID:16220976] |
| ChEMBL | Affinity for rat Muscarinic acetylcholine receptor M3 | B | 9.02 | pKi | 0.95 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2093-2096 [PMID:15808475] |
| Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26] | ||||||||
| ChEMBL | Antagonism in muscarinic M3 receptor in guinea pig left atria | F | 7.1 | pKd | 79.43 | nM | Kd | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting | B | 8.44 | pKi | 3.63 | nM | Ki | J Med Chem (2012) 55: 1783-1787 [PMID:22243489] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
J Med Chem (2012) 55: 1783-7 [PMID:22243489]; Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605] |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.56 | pKi | 0.28 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.7 | pIC50 | 1.99 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting | B | 7.85 | pKi | 14.13 | nM | Ki | J Med Chem (2012) 55: 1783-1787 [PMID:22243489] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - |
J Med Chem (2012) 55: 1783-7 [PMID:22243489]; Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605] |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.64 | pKi | 2.31 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.49 | pIC50 | 3.22 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.59 | pKi | 2573.7 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.59 | pIC50 | 2595.1 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.3 | pKi | 504 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.1 | pIC50 | 792 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 7.99 | pKi | 10.2 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | B | 7.62 | pIC50 | 24.2 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
| ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes | F | 4.79 | pIC50 | 16100 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
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]
