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Compound Detail

CHEMBL3982377

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COc1ccc(C2=C(c3ccc(C)cc3)C(=O)N(Cc3ccc(S(C)(=O)=O)cc3)C2=O)cc1OC

Basic Information

ChEMBL ID CHEMBL3982377
Phase Preclinical
Structure Type MOL
InChI Key SXJKRYTWQJBMKS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
3.90
ALogP
6
HBA
0
HBD
90.0
PSA (Ų)
0.47
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25NO6S
MW 491.57
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.33 7.33 46.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 46.3 nM 7.33 Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of pac... 27750197

Literature References

PubMed DOI Target Context # Activities
27750197 10.1016/j.ejmech.2016.09.070 Unchecked 2
27750197 10.1016/j.ejmech.2016.09.070 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine