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Compound Detail

CHEMBL4175725

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CC(C)(O)CCCn1c(Cn2nc(S(C)(=O)=O)c3ccncc32)nc2cc(Cl)ccc21

Basic Information

ChEMBL ID CHEMBL4175725
Phase Preclinical
Structure Type MOL
InChI Key XPHPTPUAKPYADB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.0
MW (Da)
3.44
ALogP
8
HBA
1
HBD
102.9
PSA (Ų)
0.45
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24ClN5O3S
MW 461.98
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.37

Activity Summary

EC50 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fusion glycoprotein F0
CHEMBL2364165
EC50 8.15 8.15 7.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 552.0 ng.hr.mL-1 Mus musculus
AUC 809.0 ng.hr.mL-1 Mus musculus
CL 60.4 mL.min-1.kg-1 Mus musculus
Cmax 2813.97 nM Mus musculus
Cmax 735.96 nM Mus musculus
F 29.3 % Mus musculus
T1/2 0.242 hr Mus musculus
T1/2 5.11 hr Mus musculus
Tmax 0.25 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28772235 10.1016/j.ejmech.2017.07.032 Mus musculus 10
28772235 10.1016/j.ejmech.2017.07.032 ADMET 3
28772235 10.1016/j.ejmech.2017.07.032 Fusion glycoprotein F0 2
28772235 10.1016/j.ejmech.2017.07.032 No relevant target 2
28772235 10.1016/j.ejmech.2017.07.032 HEp-2 1

Data from ChEMBL 36 via Core Engine