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Compound Detail

CHEMBL392006

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O=C(N[C@H]1CN(C(=O)OCC2c3ccccc3-c3ccccc32)C[C@H]1NC(=O)c1ccc2c(Cl)c[nH]c2c1)c1ccc(-n2ccccc2=O)cc1

Basic Information

ChEMBL ID CHEMBL392006
Phase Preclinical
Structure Type MOL
InChI Key ZRTHJIZWSMOBGG-MPQUPPDSSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

698.2
MW (Da)
6.13
ALogP
6
HBA
3
HBD
125.5
PSA (Ų)
0.19
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H32ClN5O5
MW 698.18
Aromatic Rings 6
Heavy Atoms 51
NP-Likeness -0.71

Activity Summary

Ki 1 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 6.79 6.79 163.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL - - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 163.0 nM 6.79 Inhibition of human factor 10a 17643988

Literature References

PubMed DOI Target Context # Activities
17643988 10.1016/j.bmcl.2007.07.020 Coagulation factor X 1
17643988 10.1016/j.bmcl.2007.07.020 Plasma 1
17643988 10.1016/j.bmcl.2007.07.020 Liver microsomes 1
17643988 10.1016/j.bmcl.2007.07.020 ADMET 1

Data from ChEMBL 36 via Core Engine