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Compound Detail

CHEMBL402935

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CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1ccccc1)NS(=O)(=O)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL402935
Phase Preclinical
Structure Type BOTH
InChI Key HYAFCDGYRQSGGV-MRLUPLGUSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

655.9
MW (Da)
2.34
ALogP
8
HBA
6
HBD
196.2
PSA (Ų)
0.05
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H41N7O5S2
MW 655.85
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.47

Activity Summary

IC50 3 meas. best 6.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor VII
CHEMBL3991
IC50 6.52 6.52 300.0 1
Coagulation factor X
CHEMBL244
IC50 6.42 6.42 380.0 1
Prothrombin
CHEMBL204
IC50 4.72 4.72 19000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor VII IC50 = 300.0 nM 6.52 Inhibition of human factor 7a 18053726
Coagulation factor X IC50 = 380.0 nM 6.42 Inhibition of human factor 10a 18053726
Prothrombin IC50 = 19000.0 nM 4.72 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor X 1
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor VII 1

Data from ChEMBL 36 via Core Engine