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Compound Detail

CHEMBL28968

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CC(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)c1nc2ccccc2o1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL28968
Phase Preclinical
Structure Type BOTH
InChI Key QFYJREBHHIAAGF-DKTLSSGOSA-N
Parent Compound CHEMBL1178471
Active Moiety CHEMBL1178471
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

661.8
MW (Da)
3.18
ALogP
7
HBA
5
HBD
194.8
PSA (Ų)
0.05
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H40F3N7O7
MW 775.79
Aromatic Rings 5
Heavy Atoms 49
NP-Likeness -0.07

Activity Summary

IC50 3 meas. best 8.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
IC50 8.19 8.19 6.4 1
Plasminogen
CHEMBL3204
IC50 7.85 7.85 14.2 1
Unchecked
CHEMBL612545
IC50 7.54 7.54 29.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 IC50 = 6.4 nM 8.19 Inhibitory concentration against trypsin. -
Plasminogen IC50 = 14.2 nM 7.85 Inhibitory concentration against plasmin. -
Unchecked IC50 = 29.0 nM 7.54 Inhibitory concentration against factor Xa(FXa). -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00227-8 Prothrombin 1
- 10.1016/S0960-894X(97)00227-8 Unchecked 1
- 10.1016/S0960-894X(97)00227-8 Serine protease 1 1
- 10.1016/S0960-894X(97)00227-8 Plasminogen 1

Data from ChEMBL 36 via Core Engine