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Compound Detail

CHEMBL3263754

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COc1nc(C2=NN(c3ccc(C#N)c(C)n3)[C@@H](C3CCCC3)C2)ccc1C(=O)O

Basic Information

ChEMBL ID CHEMBL3263754
Phase Preclinical
Structure Type MOL
InChI Key OQPWNIVCEUVXQA-LJQANCHMSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
3.54
ALogP
7
HBA
1
HBD
111.7
PSA (Ų)
0.81
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O3
MW 405.46
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.05

Activity Summary

IC50 4 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mineralocorticoid receptor
CHEMBL1994
IC50 8.12 8.12 7.6 1
Progesterone receptor
CHEMBL208
IC50 5.8 5.8 1590.0 1
Glucocorticoid receptor
CHEMBL2034
IC50 5.17 5.17 6800.0 1
Androgen receptor
CHEMBL1871
IC50 5.04 5.04 9050.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24738581 10.1021/jm500206r No relevant target 2
24738581 10.1021/jm500206r Mineralocorticoid receptor 1
24738581 10.1021/jm500206r Unchecked 1
24738581 10.1021/jm500206r Progesterone receptor 1
24738581 10.1021/jm500206r Glucocorticoid receptor 1
24738581 10.1021/jm500206r Androgen receptor 1

Data from ChEMBL 36 via Core Engine