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Compound Detail

CHEMBL158635

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COc1ccc2c(=O)c(Cn3ccnc3)c(-c3ccccc3)oc2c1

Basic Information

ChEMBL ID CHEMBL158635
Phase Preclinical
Structure Type MOL
InChI Key IXJJJDBWGBTNJP-UHFFFAOYSA-N
3
Targets
8
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

332.4
MW (Da)
3.71
ALogP
5
HBA
0
HBD
57.3
PSA (Ų)
0.57
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16N2O3
MW 332.36
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.37

Activity Summary

IC50 8 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 11B1, mitochondrial
CHEMBL1908
IC50 7.1 7.1 79.0 1
Cytochrome P450 11B2, mitochondrial
CHEMBL2722
IC50 6.91 6.91 124.0 1
Aromatase
CHEMBL1978
IC50 6.26 6.26 549.5 6

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11262078 10.1021/jm000955s Aromatase 3
16854084 10.1021/jm060186y Aromatase 2
18763754 10.1021/jm800683c Cytochrome P450 11B2, mitochondrial 2
11262078 10.1021/jm000955s Steroid 17-alpha-hydroxylase/17,20 lyase 1
16854084 10.1021/jm060186y Steroid 17-alpha-hydroxylase/17,20 lyase 1
16279787 10.1021/jm058042r Aromatase 1
19072235 10.1021/jm800945c Aromatase 1
18763754 10.1021/jm800683c Cytochrome P450 11B1, mitochondrial 1
18763754 10.1021/jm800683c Unchecked 1
28622580 10.1016/j.ejmech.2017.05.041 Aromatase 1

Data from ChEMBL 36 via Core Engine