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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| 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] |
| ChEMBL | Antagonist activity at M3 receptor (unknown origin) | B | 7.62 | pEC50 | 24 | nM | EC50 | Bioorg Med Chem Lett (2023) 80: 129048-129048 [PMID:36368496] |
| 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: 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 | 4.5 | 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 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]
