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Compound Detail

CHEMBL379465

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C[C@@H]1CN(c2ccc(C#N)c(C(F)(F)F)c2)[C@@H](C)CN1C(=O)Nc1ccc(N)nc1

Basic Information

ChEMBL ID CHEMBL379465
Phase Preclinical
Structure Type MOL
InChI Key PWOHOJWLXMLZQL-QWHCGFSZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

418.4
MW (Da)
3.69
ALogP
5
HBA
2
HBD
98.3
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 C20H21F3N6O
MW 418.42
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.43 6.43 370.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 370.0 nM 6.43 Inhibition of AR mediated transcriptional activation using reporter assay 16420057

Literature References

PubMed DOI Target Context # Activities
16420057 10.1021/jm050293c Androgen receptor 1
16420057 10.1021/jm050293c Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine