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Compound Detail

CHEMBL435761

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N=C(N)c1cccc([C@@H]2CN(Cc3ccc(-c4ccccc4S(N)(=O)=O)cc3)C[C@H]2C(=O)O)c1.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL435761
Phase Preclinical
Structure Type MOL
InChI Key WSEDDIHAZSWMIB-VSIGASKDSA-N
Parent Compound CHEMBL1185835
Active Moiety CHEMBL1185835
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

478.6
MW (Da)
2.59
ALogP
5
HBA
4
HBD
150.6
PSA (Ų)
0.30
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28F6N4O8S
MW 706.62
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.66

Activity Summary

Ki 1 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 600.0 nM 6.22 Binding affinity against Coagulation factor X in an enzyme inhibition assay. 10328312

Literature References

PubMed DOI Target Context # Activities
10328312 10.1016/s0960-894x(99)00164-x Coagulation factor X 1

Data from ChEMBL 36 via Core Engine