oxybutynin [Ligand Id: 359] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1231 (Contimin 2.5, Contimin 5, Cystrin, Ditropan, Ditropan xl, Kentera, Kentera (previously oxybutynin nicobrand), Lyrinel xl, Oxibutinina, Oxybutynin, Oxybutynine, 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 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]
