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Compound Detail

CHEMBL4068008

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CCOc1nccc2c1[C@H](c1ccc(C#N)cc1OC)C(C#N)=C(C)N2

Basic Information

ChEMBL ID CHEMBL4068008
Phase Preclinical
Structure Type MOL
InChI Key ANOXKDNMHLYCBG-GOSISDBHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
3.72
ALogP
6
HBA
1
HBD
91.0
PSA (Ų)
0.91
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 C20H18N4O2
MW 346.39
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.13

Activity Summary

IC50 4 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 7.33 7.33 47.0 1
Androgen receptor
CHEMBL1871
IC50 5.55 5.55 2800.0 1
Progesterone receptor
CHEMBL208
IC50 5.27 5.27 5400.0 1
Glucocorticoid receptor
CHEMBL2034
IC50 5.16 5.16 6900.0 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