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Compound Detail

CHEMBL601216

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CS(=O)(=O)c1ccccc1-c1ccc(NC(=O)c2cc(C(F)(F)F)nn2-c2cccc(CNC(=O)CN)c2)c(F)c1

Basic Information

ChEMBL ID CHEMBL601216
Phase Preclinical
Structure Type MOL
InChI Key QRYMLCSUZBXJMU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

589.6
MW (Da)
3.93
ALogP
7
HBA
3
HBD
136.2
PSA (Ų)
0.27
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23F4N5O4S
MW 589.57
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.81

Activity Summary

Ki 2 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.05 8.05 9.0 1
Trypsin
CHEMBL2095204
Ki 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 9.0 nM 8.05 Inhibition of human factor 10a 20100660
Trypsin Ki = 1200.0 nM 5.92 Inhibition of human trypsin 20100660

Literature References

PubMed DOI Target Context # Activities
20100660 10.1016/j.bmcl.2010.01.011 Coagulation factor X 1
20100660 10.1016/j.bmcl.2010.01.011 Prothrombin 1
20100660 10.1016/j.bmcl.2010.01.011 Trypsin 1

Data from ChEMBL 36 via Core Engine