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Compound Detail

CHEMBL2107687

VALETHAMATE BROMIDE
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CCC(C)C(C(=O)OCC[N+](C)(CC)CC)c1ccccc1.[Br-]

Basic Information

ChEMBL ID CHEMBL2107687
Name VALETHAMATE BROMIDE
Phase Preclinical
Structure Type MOL
InChI Key CEJGGHKJHDHLAZ-UHFFFAOYSA-M
Parent Compound CHEMBL2111176
Active Moiety CHEMBL2111176

Known Names

Epidosin Resitan Valethamate bromide
8
Targets
15
Activities
2
Assay Types
0
PK Parameters
1
Publications
3
Known Names

Molecular Properties

306.5
MW (Da)
3.85
ALogP
2
HBA
0
HBD
26.3
PSA (Ų)
0.51
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Racemic

Extended Properties

Molecular Formula C19H32BrNO2
MW 386.37
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness 0.04

Activity Summary

IC50 8 meas. best 7.92
Ki 7 meas. best 8.56

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 8.56 8.56 2.8 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 8.44 8.44 3.7 1
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 8.25 8.25 5.6 1
Muscarinic acetylcholine receptor M1
CHEMBL216
IC50 7.92 7.92 12.0 1
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 7.72 7.72 19.0 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 7.62 7.62 24.0 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
IC50 7.58 7.58 26.0 1
Muscarinic acetylcholine receptor M3
CHEMBL245
IC50 7.58 7.58 26.0 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
IC50 7.47 7.47 34.0 1
Muscarinic acetylcholine receptor M2
CHEMBL211
IC50 7.26 7.26 55.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 6.7 6.7 200.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 6.61 6.61 248.5 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
IC50 6.32 6.32 475.0 1
Unchecked
CHEMBL612545
Ki 5.52 5.52 3013.0 1
Unchecked
CHEMBL612545
IC50 5.47 5.47 3389.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor M1 Ki = 2.78 nM 8.56 DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M4 Ki = 3.669 nM 8.44 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M3 Ki = 5.585 nM 8.25 DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M1 IC50 = 12.0 nM 7.92 DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M2 Ki = 19.0 nM 7.72 DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M5 Ki = 24.0 nM 7.62 DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M3 IC50 = 26.0 nM 7.58 DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M4 IC50 = 26.0 nM 7.58 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M5 IC50 = 34.0 nM 7.47 DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Muscarinic acetylcholine receptor M2 IC50 = 55.0 nM 7.26 DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Sigma non-opioid intracellular receptor 1 Ki = 200.0 nM 6.7 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) -
Cytochrome P450 2D6 IC50 = 248.5 nM 6.61 DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) -
Sigma non-opioid intracellular receptor 1 IC50 = 475.0 nM 6.32 DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) -
Unchecked Ki = 3013.0 nM 5.52 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -
Unchecked IC50 = 3389.0 nM 5.47 DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand:... -

Literature References

PubMed DOI Target Context # Activities
- 10.1101/2020.04.03.023846 SARS-CoV-2 1

Data from ChEMBL 36 via Core Engine