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Compound Detail

CHEMBL3314487

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COCCCOc1cccc([C@H]2NC(=S)Nc3c2oc2ccccc32)c1

Basic Information

ChEMBL ID CHEMBL3314487
Phase Preclinical
Structure Type MOL
InChI Key QWHBACLOOIUCGE-QGZVFWFLSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
4.24
ALogP
4
HBA
2
HBD
55.7
PSA (Ų)
0.50
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H20N2O3S
MW 368.46
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.49

Activity Summary

IC50 2 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily A member 1
CHEMBL5160
IC50 6.64 6.64 230.0 1
Transient receptor potential cation channel subfamily A member 1
CHEMBL6007
IC50 6.23 6.23 590.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 90.0 mL.min-1.g-1 Homo sapiens
CL 350.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24953819 10.1016/j.bmcl.2014.05.069 Transient receptor potential cation channel subfamily A member 1 4
24953819 10.1016/j.bmcl.2014.05.069 No relevant target 2
24953819 10.1016/j.bmcl.2014.05.069 Liver microsome 2
24953819 10.1016/j.bmcl.2014.05.069 ADMET 1

Data from ChEMBL 36 via Core Engine