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Compound Detail

CHEMBL4096901

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CCOc1ncc(C)c2c1[C@H](c1ccc(C#N)cc1OC)C(C#N)=C(C)N2

Basic Information

ChEMBL ID CHEMBL4096901
Phase Preclinical
Structure Type MOL
InChI Key YWJJBRLFZBLSNJ-GOSISDBHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

360.4
MW (Da)
4.02
ALogP
6
HBA
1
HBD
91.0
PSA (Ų)
0.89
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 C21H20N4O2
MW 360.42
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.16

Activity Summary

IC50 4 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 7.58 7.58 26.0 1
Androgen receptor
CHEMBL1871
IC50 5.62 5.62 2400.0 1
Progesterone receptor
CHEMBL208
IC50 5.38 5.38 4200.0 1
Glucocorticoid receptor
CHEMBL2034
IC50 5.24 5.24 5800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28051871 10.1021/acs.jmedchem.6b01065 Mineralocorticoid receptor 1
28051871 10.1021/acs.jmedchem.6b01065 Glucocorticoid receptor 1
28051871 10.1021/acs.jmedchem.6b01065 Androgen receptor 1
28051871 10.1021/acs.jmedchem.6b01065 Progesterone receptor 1

Data from ChEMBL 36 via Core Engine