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Compound Detail

CHEMBL205288

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Nc3ccc(-c4ccccc4CN4CC[C@H](N)C4)cc3F)cc12

Basic Information

ChEMBL ID CHEMBL205288
Phase Preclinical
Structure Type MOL
InChI Key YHIZCAWNRNQWMF-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

579.6
MW (Da)
5.21
ALogP
8
HBA
3
HBD
128.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25F4N7O2
MW 579.56
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.65

Activity Summary

Ki 1 meas. best 9.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.27 9.27 0.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.54 nM 9.27 Binding affinity to human factor 10a 16434195

Literature References

PubMed DOI Target Context # Activities
16434195 10.1016/j.bmcl.2006.01.010 Coagulation factor X 1
16434195 10.1016/j.bmcl.2006.01.010 Caco-2 1
16434195 10.1016/j.bmcl.2006.01.010 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine