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Compound Detail

CHEMBL255776

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O=C1[C@H]2C3CCC(C3)N2C(=O)N1c1cccc(C(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL255776
Phase Preclinical
Structure Type MOL
InChI Key AZEYWBIKLUFKOJ-YPXMJKPUSA-N
1
Targets
2
Activities
2
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

310.3
MW (Da)
3.02
ALogP
2
HBA
0
HBD
40.6
PSA (Ų)
0.75
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H13F3N2O2
MW 310.27
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -1.07

Activity Summary

IC50 1 meas. best 6.89
Ki 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
Ki 7.68 7.68 21.0 1
Androgen receptor
CHEMBL1871
IC50 6.89 6.89 130.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3537.08 ng.hr.mL-1 Mus musculus
Cmax 1740.0 nM Mus musculus
Tmax 0.5 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18291644 10.1016/j.bmcl.2008.02.006 Mus musculus 3
18291644 10.1016/j.bmcl.2008.02.006 Androgen receptor 2

Data from ChEMBL 36 via Core Engine