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Compound Detail

CHEMBL280155

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C[C@]12CCC(=O)C=C1NCC1C2CC[C@@]2(C)C1CC[C@@H]2C(=O)Nc1ccccc1

Basic Information

ChEMBL ID CHEMBL280155
Phase Preclinical
Structure Type MOL
InChI Key NEXQLYFTKBAWDD-KFFMOSLCSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
4.54
ALogP
3
HBA
2
HBD
58.2
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32N2O2
MW 392.54
Aromatic Rings 1
Heavy Atoms 29
NP-Likeness 0.90

Activity Summary

Ki 4 meas. best 8.0
IC50 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
3-oxo-5-alpha-steroid 4-dehydrogenase 2
CHEMBL1856
IC50 8.85 8.85 1.4 2
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1
CHEMBL1958
Ki 8.0 8.0 10.0 1
Unchecked
CHEMBL612545
Ki 8.0 8.0 10.0 1
3-oxo-5-alpha-steroid 4-dehydrogenase 1
CHEMBL1787
Ki 6.62 6.62 240.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9135028 10.1021/jm960697s 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
9135028 10.1021/jm960697s 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
9135028 10.1021/jm960697s 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1 1
7629802 10.1021/jm00014a015 3-oxo-5-alpha-steroid 4-dehydrogenase 1 1
7629802 10.1021/jm00014a015 3-oxo-5-alpha-steroid 4-dehydrogenase 2 1
7629802 10.1021/jm00014a015 Unchecked 1

Data from ChEMBL 36 via Core Engine