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Compound Detail

CHEMBL3589384

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N#Cc1ccc(N2C(=O)[C@]3(CCOC3)N(c3ccc(C(=O)O)c(F)c3)C2=S)cc1C(F)(F)F

Basic Information

ChEMBL ID CHEMBL3589384
Phase Preclinical
Structure Type MOL
InChI Key GRFRYIRPPUMEGU-HXUWFJFHSA-N
0
Targets
0
Activities
0
Assay Types
19
PK Parameters
3
Publications
0
Known Names

Molecular Properties

479.4
MW (Da)
3.71
ALogP
5
HBA
1
HBD
93.9
PSA (Ų)
0.53
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 C21H13F4N3O4S
MW 479.41
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.18

Pharmacokinetic Data

Parameter Value Units Species
AUC 509.0 ng.hr.mL-1 Rattus norvegicus
AUC 743.0 ng.hr.mL-1 Rattus norvegicus
AUC 497.0 ng.hr.mL-1 Rattus norvegicus
AUC 716.0 ng.hr.mL-1 Rattus norvegicus
CL 33.33 mL.min-1.kg-1 Rattus norvegicus
CL 116.67 mL.min-1.kg-1 Rattus norvegicus
Cmax 2455.1 nM Rattus norvegicus
Cmax 481.84 nM Rattus norvegicus
F 29.0 % Rattus norvegicus
MRT 3.5 hr Rattus norvegicus
MRT 0.5 hr Rattus norvegicus
MRT 4.2 hr Rattus norvegicus
MRT 0.8 hr Rattus norvegicus
T1/2 3.3 hr Rattus norvegicus
T1/2 4.0 hr Rattus norvegicus
Tmax 0.083 hr Rattus norvegicus
Tmax 0.42 hr Rattus norvegicus
Vd 8.0 L.kg-1 Rattus norvegicus
Vd 38.4 L.kg-1 Rattus norvegicus

Literature References

PubMed DOI Target Context # Activities
26046313 10.1016/j.ejmech.2015.05.039 Rattus norvegicus 23
26046313 10.1016/j.ejmech.2015.05.039 Androgen receptor 1
26046313 10.1016/j.ejmech.2015.05.039 LNCaP 1

Data from ChEMBL 36 via Core Engine