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Compound Detail

CHEMBL265087

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CN1CCN(Cc2ccccc2-c2ccc(N3CCc4c(C(F)(F)F)nn(-c5ccc6onc(N)c6c5)c4C3=O)cc2)CC1

Basic Information

ChEMBL ID CHEMBL265087
Phase Preclinical
Structure Type MOL
InChI Key ASRYKRVWPDUVJA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

601.6
MW (Da)
5.23
ALogP
8
HBA
1
HBD
96.7
PSA (Ų)
0.29
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H30F3N7O2
MW 601.63
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -1.21

Activity Summary

Ki 2 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.15 9.15 0.7 1
Prothrombin
CHEMBL204
Ki 6.64 6.64 230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.71 nM 9.15 Binding affinity to human F10a 16730984
Prothrombin Ki = 230.0 nM 6.64 Binding affinity to human F2a 16730984

Literature References

PubMed DOI Target Context # Activities
16730984 10.1016/j.bmcl.2006.02.069 Prothrombin 1
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor VII/tissue factor 1
16730984 10.1016/j.bmcl.2006.02.069 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine