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Compound Detail

CHEMBL271047

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N=C(N)NCCC[C@H](NC(=O)CNC(=O)[C@@H](CCCNC(=N)N)NS(=O)(=O)CCc1ccccc1)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL271047
Phase Preclinical
Structure Type BOTH
InChI Key FFYWSDGJFSQDBD-FCHUYYIVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

672.8
MW (Da)
0.14
ALogP
9
HBA
9
HBD
258.1
PSA (Ų)
0.04
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H40N10O5S2
MW 672.84
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.81

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.7 8.7 2.0 1
Plasma kallikrein
CHEMBL2000
IC50 7.54 7.54 29.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 2.0 nM 8.7 Inhibition of human factor 10a 18053726
Plasma kallikrein IC50 = 29.0 nM 7.54 Inhibition of kallikrein 18053726

Literature References

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

Data from ChEMBL 36 via Core Engine