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Compound Detail

CHEMBL201327

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COC(=O)c1ccc(NC(=O)N2C[C@H](C)N(c3ccc(C#N)c(C(F)(F)F)c3)C[C@H]2C)cn1

Basic Information

ChEMBL ID CHEMBL201327
Phase Preclinical
Structure Type MOL
InChI Key IQMALUHRLDMWJS-UONOGXRCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

461.4
MW (Da)
3.89
ALogP
6
HBA
1
HBD
98.6
PSA (Ų)
0.70
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22F3N5O3
MW 461.44
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.62

Activity Summary

IC50 1 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.33 6.33 470.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 470.0 nM 6.33 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