oxybutynin [Ligand Id: 359] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1231 (Oxytrol, Contimin 2.5, Contimin 5, Anturol, Oxybutynin, Cystrin, Kentera, Ditropan xl, Promictuline, Urimin, Lyrinel xl, Oxytrol for women, Ditropan)
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • Lethal(3)malignant brain tumor-like protein 1 in Human [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468]
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  • L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7]
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  • Lethal(3)malignant brain tumor-like protein 4 in Human [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
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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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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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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 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]

ChEMBL data shown on this page come from version 28:

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]