solifenacin [Ligand Id: 7483] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1734 (NSC-759144, Solifenacin, Vesicare)
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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]
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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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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382P51787]
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  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
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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) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform F 5.8 pIC50 1584.89 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 6.6 pIC50 251.19 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]
ChEMBL Displacement of [3H]NMS from recombinant human muscarinic M1 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method B 7.29 pKi 51.29 nM Ki Eur J Med Chem (2017) 137: 327-337 [PMID:28609709]
GtoPdb - - 7.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2002) 366: 97-103 [PMID:12122494];
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]
GtoPdb - - 7.2 pIC50 63.5 nM IC50 Bioorg Med Chem Lett (2011) 21: 3457-61 [PMID:21524581]
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
GtoPdb - - 8 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 pKi 10 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 Displacement of [3H]NMS from recombinant human muscarinic M2 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method B 6.92 pKi 120.23 nM Ki Eur J Med Chem (2017) 137: 327-337 [PMID:28609709]
GtoPdb - - 7.1 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2002) 366: 97-103 [PMID:12122494];
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]
GtoPdb - - 6.24 pIC50 573 nM IC50 Bioorg Med Chem Lett (2011) 21: 3457-61 [PMID:21524581]
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 6.92 pKi 120 nM Ki J. Med. Chem. (2005) 48: 6597-6606 [PMID:16220976]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method B 7.88 pKi 13.18 nM Ki Eur J Med Chem (2017) 137: 327-337 [PMID:28609709]
GtoPdb - - 8 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2002) 366: 97-103 [PMID:12122494];
Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]
GtoPdb - - 6.88 pIC50 130.8 nM IC50 Bioorg Med Chem Lett (2011) 21: 3457-61 [PMID:21524581]
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 pKi 10 nM Ki J. Med. Chem. (2005) 48: 6597-6606 [PMID:16220976]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb - - 6.8 pKi - - - Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]
ChEMBL Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method B 6.89 pKi 128.82 nM Ki Eur J Med Chem (2017) 137: 327-337 [PMID:28609709]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
GtoPdb - - 7.2 pKi - - - Br J Pharmacol (2010) 160: 1119-27 [PMID:20590605]
ChEMBL Displacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method B 7.36 pKi 43.65 nM Ki Eur J Med Chem (2017) 137: 327-337 [PMID:28609709]
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 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]
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 (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 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]
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 4.5 pIC50 31622.78 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 4.3 pIC50 50118.72 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]

ChEMBL data shown on this page come from version 31:

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]