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Compound Detail

CHEMBL396087

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COc1ccc(-n2nc(-n3cnnn3)c3c2C(=O)N(c2ccc(-c4ccccc4CN4CC[C@@H](O)C4)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL396087
Phase Preclinical
Structure Type MOL
InChI Key HDWBKYNEUKAHLE-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

562.6
MW (Da)
3.29
ALogP
10
HBA
1
HBD
114.4
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H30N8O3
MW 562.63
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -1.35

Activity Summary

Ki 1 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.64 8.64 2.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 2.3 nM 8.64 Binding affinity to human F10a 17914785

Literature References

PubMed DOI Target Context # Activities
17914785 10.1021/jm070245n Coagulation factor X 1
17914785 10.1021/jm070245n Prothrombin 1
17914785 10.1021/jm070245n Plasma 1
17914785 10.1021/jm070245n Trypsin 1

Data from ChEMBL 36 via Core Engine