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Compound Detail

CHEMBL403904

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CCNC(=O)N1CC[C@H](NC(=O)c2cc3cc(Cl)ccc3[nH]2)[C@H](NC(=O)c2nc3c(s2)CN(C)CC3)C1

Basic Information

ChEMBL ID CHEMBL403904
Phase Preclinical
Structure Type MOL
InChI Key GWBGYFMKMILOEX-FXAWDEMLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

544.1
MW (Da)
2.60
ALogP
6
HBA
4
HBD
122.5
PSA (Ų)
0.39
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30ClN7O3S
MW 544.08
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.64

Activity Summary

IC50 1 meas. best 8.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.11 8.11 7.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 7.8 nM 8.11 Inhibition of human factor 10a 18039572

Literature References

PubMed DOI Target Context # Activities
18039572 10.1016/j.bmcl.2007.11.037 Rattus norvegicus 4
18039572 10.1016/j.bmcl.2007.11.037 No relevant target 1
18039572 10.1016/j.bmcl.2007.11.037 Coagulation factor X 1
18039572 10.1016/j.bmcl.2007.11.037 Plasma 1

Data from ChEMBL 36 via Core Engine