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Compound Detail

CHEMBL4217036

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COc1ccc(F)cc1S(=O)(=O)Nc1cncc(C(N)=O)c1

Basic Information

ChEMBL ID CHEMBL4217036
Phase Preclinical
Structure Type MOL
InChI Key MRXCAMVVHKTMGD-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
6
PK Parameters
2
Publications
0
Known Names

Molecular Properties

325.3
MW (Da)
1.13
ALogP
5
HBA
2
HBD
111.4
PSA (Ų)
0.86
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H12FN3O4S
MW 325.32
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -2.07

Activity Summary

IC50 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alkaline phosphatase, tissue-nonspecific isozyme
CHEMBL5979
IC50 7.72 7.34 19.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 141000.0 ng.hr.mL-1 Mus musculus
CL 16.8 mL.min-1.kg-1 Mus musculus
Cmax 193655.48 nM Mus musculus
F 100.0 % Mus musculus
T1/2 3.7 hr Mus musculus
Vd 0.88 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29174347 10.1016/j.bmcl.2017.11.024 Mus musculus 6
29174347 10.1016/j.bmcl.2017.11.024 Alkaline phosphatase, tissue-nonspecific isozyme 2

Data from ChEMBL 36 via Core Engine