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Compound Detail

CHEMBL1734

SOLIFENACIN
💊 Approved Drug
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💊 Approved Drug
O=C(O[C@H]1CN2CCC1CC2)N1CCc2ccccc2[C@@H]1c1ccccc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1734
Name SOLIFENACIN
Phase Approved
Structure Type MOL
InChI Key FBOUYBDGKBSUES-VXKWHMMOSA-N
Therapeutic ✓ Yes

Known Names

NSC-759144 Solifenacin Solifenacina Solifenacine Vesicare
15
Targets
20
Activities
3
Assay Types
15
PK Parameters
20
Publications
5
Known Names
5
Indications

Molecular Properties

362.5
MW (Da)
3.86
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.81
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2004
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral

Flags

Natural Product
USAN Stem -fenacin
USAN Year 2001

Extended Properties

Molecular Formula C23H26N2O2
MW 362.47
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.06

Indications

Polyuria Urinary Incontinence Prostatic Hyperplasia Urinary Bladder, Overactive Urinary Incontinence, Urge

ATC Classification

G04BD08
solifenacin
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: UROLOGICALS

Activity Summary

IC50 9 meas. best 7.62
Ki 8 meas. best 8.0
EC50 3 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL320
 Ki 8.0 8.0 10.0 1
Muscarinic acetylcholine receptor M1
CHEMBL276
 Ki 8.0 8.0 10.0 1
Muscarinic acetylcholine receptor M3
CHEMBL245
 Ki 7.88 7.88 13.2 1
Muscarinic acetylcholine receptor M3
CHEMBL245
 EC50 7.62 7.62 24.0 1
Muscarinic acetylcholine receptor M3
CHEMBL245
 IC50 7.62 7.62 24.0 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
 Ki 7.36 7.36 43.6 1
Muscarinic acetylcholine receptor M1
CHEMBL216
 Ki 7.29 7.29 51.3 1
Muscarinic acetylcholine receptor M2
CHEMBL211
 Ki 6.92 6.92 120.2 1
Muscarinic acetylcholine receptor M2
CHEMBL309
 Ki 6.92 6.92 120.0 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
 Ki 6.89 6.89 128.8 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
 IC50 6.6 6.3233 251.2 3
Unchecked
CHEMBL612545
 EC50 5.89 5.89 1300.0 2
Voltage-gated L-type calcium channel
CHEMBL2095229
 IC50 5.37 5.37 4300.0 1
Voltage-dependent L-type calcium channel subunit alpha-1C
CHEMBL1940
 IC50 5.2 5.2 6309.6 1
Sodium channel protein type 5 subunit alpha
CHEMBL1980
 IC50 5.2 5.2 6309.6 1
Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK)
CHEMBL2221347
 IC50 4.5 4.5 31622.8 1
A-type voltage-gated potassium channel KCND3
CHEMBL1964
 IC50 4.3 4.3 50118.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.1 mL.min-1.kg-1 Homo sapiens
CL 2.0 mL.min-1.kg-1 Homo sapiens
CL 2.1 mL.min-1.kg-1 Homo sapiens
CL 2.1 mL.min-1.kg-1 Homo sapiens
Fu 0.02 - Homo sapiens
Fu 0.02 - Homo sapiens
Fu 0.017 - Homo sapiens
Fu 0.016 - Macaca fascicularis
Fu 0.018 - Canis lupus familiaris
Fu 0.014 - Cavia porcellus
Fu 0.016 - Mus musculus
Fu 0.015 - Rattus norvegicus
Fu 0.019 - Rattus norvegicus
MRT 65.0 hr Homo sapiens
T1/2 52.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor M3 Ki = 10.0 nM 8.0 Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 usi... 16220976
Muscarinic acetylcholine receptor M1 Ki = 10.0 nM 8.0 Binding affinity for rat cortex muscarinic acetylcholine receptor M1 using [3H]p... 16220976
Muscarinic acetylcholine receptor M3 Ki = 13.18 nM 7.88 Displacement of [3H]NMS from recombinant human muscarinic M3 receptor expressed ... 28609709
Muscarinic acetylcholine receptor M3 EC50 = 24.0 nM 7.62 Antagonist activity at M3 receptor (unknown origin) 36368496
Muscarinic acetylcholine receptor M3 IC50 = 24.0 nM 7.62 Antagonist activity at muscarinic M3 receptor (unknown origin) 34153473
Muscarinic acetylcholine receptor M5 Ki = 43.65 nM 7.36 Displacement of [3H]NMS from recombinant human muscarinic M5 receptor expressed ... 28609709
Muscarinic acetylcholine receptor M1 Ki = 51.29 nM 7.29 Displacement of [3H]NMS from recombinant human muscarinic M1 receptor expressed ... 28609709
Muscarinic acetylcholine receptor M2 Ki = 120.23 nM 6.92 Displacement of [3H]NMS from recombinant human muscarinic M2 receptor expressed ... 28609709
Muscarinic acetylcholine receptor M2 Ki = 120.0 nM 6.92 Binding affinity for rat heart muscarinic acetylcholine receptor M2 using [3H]qu... 16220976
Muscarinic acetylcholine receptor M4 Ki = 128.82 nM 6.89 Displacement of [3H]NMS from recombinant human muscarinic M4 receptor expressed ... 28609709
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 251.19 nM 6.6 Inhibition of rapid delayed inward rectifying potassium current (IKr) measured u... 25087753
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 270.0 nM 6.57 Inhibition of human ERG 36368496
Unchecked EC50 = 1300.0 nM 5.89 Increase of PGRN level in mouse microglial BV-2 cell relative to control 34153473
Unchecked EC50 = 1300.0 nM 5.89 Induction of progranulin secretion in mouse BV-2 cells 36368496
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 1584.89 nM 5.8 Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese... 25087753
Voltage-gated L-type calcium channel IC50 = 4300.0 nM 5.37 Inhibition of Cav1.2 current measured using QPatch automatic path clamp system i... 23812503
Sodium channel protein type 5 subunit alpha IC50 = 6309.57 nM 5.2 Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells ... 25087753
Voltage-dependent L-type calcium channel subunit alpha-1C IC50 = 6309.57 nM 5.2 Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary ... 25087753
Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) IC50 = 31622.78 nM 4.5 Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese ... 25087753
A-type voltage-gated potassium channel KCND3 IC50 = 50118.72 nM 4.3 Inhibition of transient outward potassium current (Ito) current in Chinese Hamst... 25087753

Literature References

PubMed DOI Target Context # Activities
20070106 10.1021/jm901371v Homo sapiens 8
16220976 10.1021/jm050099q Rattus norvegicus 5
21474681 10.1124/dmd.111.038778 Brain 5
18426954 10.1124/dmd.108.020479 ADMET 4
25087753 10.1016/j.vascn.2014.07.002 Voltage-gated inwardly rectifying potassium channel KCNH2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
26948801 10.1016/j.drudis.2016.02.015 Homo sapiens 2
19445515 10.1021/jm900403j Homo sapiens 2
20070106 10.1021/jm901371v Plasma 1
18426954 10.1124/dmd.108.020479 NON-PROTEIN TARGET 1
16220976 10.1021/jm050099q Muscarinic acetylcholine receptor M1 1
25087753 10.1016/j.vascn.2014.07.002 Voltage-dependent L-type calcium channel subunit alpha-1C 1
25087753 10.1016/j.vascn.2014.07.002 Sodium channel protein type 5 subunit alpha 1
25087753 10.1016/j.vascn.2014.07.002 Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) 1
25087753 10.1016/j.vascn.2014.07.002 A-type voltage-gated potassium channel KCND3 1
23812503 10.1038/srep02100 Voltage-gated L-type calcium channel 1
21474681 10.1124/dmd.111.038778 NON-PROTEIN TARGET 1
16220976 10.1021/jm050099q Muscarinic receptor M2 and M3 1
36368496 10.1016/j.bmcl.2022.129048 Muscarinic acetylcholine receptor M3 1
16220976 10.1021/jm050099q Muscarinic acetylcholine receptor M3 1

Data from ChEMBL 36 via Core Engine