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Compound Detail

CHEMBL4472744

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CC(C)C[C@H](NC(=O)OC1CCN(S(=O)(=O)c2ccc([N+](=O)[O-])cc2[N+](=O)[O-])CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nc2ccccc2s1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL4472744
Phase Preclinical
Structure Type MOL
InChI Key ZJURWLSJUIYUGI-SJEIDVEUSA-N
Parent Compound CHEMBL4598105
Active Moiety CHEMBL4598105
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

761.8
MW (Da)
3.04
ALogP
13
HBA
5
HBD
282.9
PSA (Ų)
0.04
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H40F3N9O12S2
MW 875.86
Aromatic Rings 3
Heavy Atoms 52
NP-Likeness -1.07

Activity Summary

IC50 2 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease hepsin
CHEMBL2079849
IC50 6.96 6.96 110.0 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31803403 10.1039/C9MD00234K Prothrombin 1
31803403 10.1039/C9MD00234K Coagulation factor X 1
31803403 10.1039/C9MD00234K Hepatocyte growth factor activator 1
31803403 10.1039/C9MD00234K Serine protease hepsin 1
31803403 10.1039/C9MD00234K Suppressor of tumorigenicity 14 protein 1

Data from ChEMBL 36 via Core Engine