tolterodine [Ligand Id: 360] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1382 (Blerone xl, Detrusitol, Detrusitol xl, Efflosomyl xl, Inconex xl, KABI 2234, KABI-2234, Mariosea xl, Neditol xl, Preblacon xl, Santizor xl, Tolterodine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | F | 6.8 | pIC50 | 158.49 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform | F | 6.9 | pIC50 | 125.89 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 7.77 | pIC50 | 16.98 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | F | 7.9 | pIC50 | 12.59 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| GtoPdb | - | - | 8.5 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M1 receptor expressed in CHO cells | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 825-827 [PMID:18042383] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Displacement of [3H]NMS from muscarinic receptor M1 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method | B | 8.85 | pKi | 1.4 | nM | Ki | J Med Chem (2018) 61: 4020-4029 [PMID:29652494] |
| 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 | 7.8 | pKd | 15.85 | nM | Kd | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| ChEMBL | Binding affinity to human muscarinic M2 receptor | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M2 receptor expressed in CHO cells | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 825-827 [PMID:18042383] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Affinity for rat Muscarinic acetylcholine receptor M2 | B | 8.16 | pKi | 6.91 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2093-2096 [PMID:15808475] |
| ChEMBL | Displacement of [3H]NMS from muscarinic receptor M2 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2018) 61: 4020-4029 [PMID:29652494] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M3 receptor expressed in CHO cells | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 825-827 [PMID:18042383] |
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay | B | 8.44 | pKi | 3.6 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2759-2763 [PMID:21075627] |
| ChEMBL | Displacement of [3H]N-methylscopolamine from human M3 receptor | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2011) 54: 6998-7002 [PMID:21863888] |
| ChEMBL | Binding affinity to human muscarinic M3 receptor | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 373-377 [PMID:16275087] |
| GtoPdb | - | - | 8.5 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | Affinity for rat Muscarinic acetylcholine receptor M3 | B | 8.15 | pKi | 7.07 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2093-2096 [PMID:15808475] |
| ChEMBL | Displacement of [3H]NMS from muscarinic receptor M3 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2018) 61: 4020-4029 [PMID:29652494] |
| 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 | 7.7 | pKd | 19.95 | 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] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 825-827 [PMID:18042383] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Displacement of [3H]NMS from muscarinic receptor M4 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method | B | 8.51 | pKi | 3.1 | nM | Ki | J Med Chem (2018) 61: 4020-4029 [PMID:29652494] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M5 receptor expressed in CHO cells | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 825-827 [PMID:18042383] |
| GtoPdb | - | - | 8.8 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]; Eur J Pharmacol (1998) 349: 285-92 [PMID:9671109] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
| ChEMBL | Displacement of [3H]NMS from muscarinic receptor M5 in Sprague-Dawley rat brain homogenates after 60 mins by liquid scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2018) 61: 4020-4029 [PMID:29652494] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | F | 4.5 | pIC50 | 31622.78 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | F | 5.2 | pIC50 | 6309.57 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| 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 | 6.84 | pIC50 | 143 | nM | IC50 | J Appl Toxicol (2012) 32: 858-866 [PMID:22761000] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform | F | 4.6 | pIC50 | 25118.86 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] | ||||||||
| ChEMBL | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform | F | 4.1 | pIC50 | 79432.82 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17] | ||||||||
| ChEMBL | Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
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]
