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Compound Detail

CHEMBL2335003

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COc1ccc(-c2nc(CN3CCc4cc(OC)c(OC)cc4C3)cs2)cc1

Basic Information

ChEMBL ID CHEMBL2335003
Phase Preclinical
Structure Type MOL
InChI Key CILWRSDWEVZXPT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
4.39
ALogP
6
HBA
0
HBD
43.8
PSA (Ų)
0.62
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 C22H24N2O3S
MW 396.51
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.35

Activity Summary

EC50 3 meas. best 5.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 5.71 5.71 1940.0 1
Multidrug resistance-associated protein 1
CHEMBL3004
EC50 5.57 5.57 2700.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 4.52 4.52 30000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23374872 10.1016/j.bmcl.2012.12.084 Caco-2 1
23374872 10.1016/j.bmcl.2012.12.084 Multidrug resistance-associated protein 1 1
23374872 10.1016/j.bmcl.2012.12.084 Broad substrate specificity ATP-binding cassette transporter ABCG2 1
23374872 10.1016/j.bmcl.2012.12.084 ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine