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Compound Detail

CHEMBL185707

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N=C(N)c1cccc(-n2nc(C(F)(F)F)cc2C(=O)Nc2ccc(-n3ccnc3)cc2)c1

Basic Information

ChEMBL ID CHEMBL185707
Phase Preclinical
Structure Type MOL
InChI Key MBUSOSLPKAWWDF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

439.4
MW (Da)
3.61
ALogP
6
HBA
3
HBD
114.6
PSA (Ų)
0.33
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16F3N7O
MW 439.40
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -2.03

Activity Summary

Ki 2 meas. best 10.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.05 10.05 0.1 1
Coagulation factor IX
CHEMBL2016
Ki 7.14 7.14 72.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.09 nM 10.05 Binding affinity towards human factor Xa 15454208
Coagulation factor IX Ki = 72.0 nM 7.14 Binding affinity towards human factor IXa 15454208

Literature References

PubMed DOI Target Context # Activities
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor X 1
15454208 10.1016/j.bmcl.2004.08.034 Coagulation factor IX and X 1

Data from ChEMBL 36 via Core Engine