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Compound Detail

CHEMBL214730

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Nc1nc2c(C(F)(F)F)nn(-c3ccc4onc(N)c4c3)c2c(O)c1-c1ccc(-c2ccccc2CN2CCC(O)CC2)cc1

Basic Information

ChEMBL ID CHEMBL214730
Phase Preclinical
Structure Type MOL
InChI Key JKTNGLROJHNUKW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

615.6
MW (Da)
5.74
ALogP
10
HBA
4
HBD
152.5
PSA (Ų)
0.19
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 C32H28F3N7O3
MW 615.62
Aromatic Rings 6
Heavy Atoms 45
NP-Likeness -0.86

Activity Summary

Ki 1 meas. best 9.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.11 9.11 0.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.77 nM 9.11 Binding affinity to human f10a 16870435

Literature References

PubMed DOI Target Context # Activities
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor X 2
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor VII/tissue factor 1

Data from ChEMBL 36 via Core Engine