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Compound Detail

CHEMBL4173941

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COc1ccc(S(=O)(=O)NCCc2c(C(c3ccc(O)cc3)c3[nH]c4ccccc4c3CCNS(=O)(=O)c3ccc(OC)cc3)[nH]c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL4173941
Phase Preclinical
Structure Type MOL
InChI Key DYWFGTKTWNULDY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

764.9
MW (Da)
6.59
ALogP
7
HBA
5
HBD
162.6
PSA (Ų)
0.08
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H40N4O7S2
MW 764.93
Aromatic Rings 7
Heavy Atoms 54
NP-Likeness -0.21

Activity Summary

IC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aromatase IC50 = 700.0 nM 6.16 Inhibition of aromatase (unknown origin) using O-benzyl fluorescein benzyl ester... 29137864

Literature References

PubMed DOI Target Context # Activities
29137864 10.1016/j.ejmech.2017.10.057 Vero 1
29137864 10.1016/j.ejmech.2017.10.057 Aromatase 1
29137864 10.1016/j.ejmech.2017.10.057 Unchecked 1

Data from ChEMBL 36 via Core Engine