tolterodine [Ligand Id: 360] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1382 (Efflosomyl xl, Neditol xl, KABI 2234, KABI-2234, Blerone xl, Inconex xl, Preblacon xl, Detrusitol xl, Santizor xl, Detrusitol, Tolterodine, Mariosea xl)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
1 CHEMBL1382_lig_chart_1 HERG Human
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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]
  • 8.85
2 CHEMBL1382_lig_chart_2 Muscarinic acetylcholine receptor M1 HumanRat
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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]
  • 8.36
3 CHEMBL1382_lig_chart_3 Muscarinic acetylcholine receptor M2 HumanRat
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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]
  • 0
4 CHEMBL1382_lig_chart_4 Muscarinic acetylcholine receptor M3 HumanRatGuinea pig
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
  • 8.51
5 CHEMBL1382_lig_chart_5 Muscarinic acetylcholine receptor M4 HumanRat
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Rat [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
  • 8.66
6 CHEMBL1382_lig_chart_6 Muscarinic acetylcholine receptor M5 HumanRat
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1382_lig_chart_7 Sodium channel protein type V alpha subunit Human
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1382_lig_chart_8 Voltage-dependent L-type calcium channel subunit alpha-1C Guinea pig
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1382_lig_chart_9 Voltage-gated L-type calcium channel alpha-1C subunit Human
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1382_lig_chart_10 Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) Human
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  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
  • This target only has 0 pki data point
  • 0
11 CHEMBL1382_lig_chart_11 Voltage-gated potassium channel subunit Kv4.3 Human
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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 Journal of Applied Toxicology (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: P15382P51787]
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 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]