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, Tolterodina, 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 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]
