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Compound Detail

CHEMBL4799175

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CCN1C(=O)N(c2ccc(F)c(C(F)(F)F)c2)C(=O)C1(C)C

Basic Information

ChEMBL ID CHEMBL4799175
Phase Preclinical
Structure Type MOL
InChI Key WMPVPVZXKSLXMJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
6
Publications
0
Known Names

Molecular Properties

318.3
MW (Da)
3.41
ALogP
2
HBA
0
HBD
40.6
PSA (Ų)
0.62
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H14F4N2O2
MW 318.27
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness -1.33

Activity Summary

IC50 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
IC50 6.85 6.85 140.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 32781.81 ng.hr.mL-1 Mus musculus
CL 30.0 mL.min-1.g-1 Homo sapiens
CL 32.0 mL.min-1.g-1 Mus musculus
Cmax 11100.0 nM Mus musculus
Tmax 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor IC50 = 140.0 nM 6.85 Inhibition of wild-type androgen receptor in human LAPC4 cells assessed as inhib... 27933964

Literature References

Data from ChEMBL 36 via Core Engine