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Compound Detail

CHEMBL392508

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CNC(=O)N1C[C@H](NC(=O)c2ccc(-n3ccccc3=O)cc2)[C@H](NC(=O)c2ccc(Cl)s2)C1

Basic Information

ChEMBL ID CHEMBL392508
Phase Preclinical
Structure Type MOL
InChI Key WDGSIXLLWZZNKD-DLBZAZTESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.0
MW (Da)
2.10
ALogP
6
HBA
3
HBD
112.5
PSA (Ų)
0.50
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 C23H22ClN5O4S
MW 499.98
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.44

Activity Summary

Ki 1 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 8.96 8.96 1.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL - nmol/mg/min Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 1.1 nM 8.96 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