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Compound Detail

CHEMBL387856

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COc1cc(Cl)cc(C(=O)Nc2ccc(Cl)cn2)c1NC(=O)c1scc(CN(C)C2=NCCCO2)c1Cl

Basic Information

ChEMBL ID CHEMBL387856
Phase Preclinical
Structure Type MOL
InChI Key PQEQQMLZYPTIEQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

582.9
MW (Da)
5.82
ALogP
8
HBA
2
HBD
105.2
PSA (Ų)
0.36
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 C24H22Cl3N5O4S
MW 582.90
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.42

Activity Summary

Ki 2 meas. best 10.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.92 10.92 0.0 1
Prothrombin
CHEMBL204
Ki 6.8 6.8 160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.012 nM 10.92 Inhibition of human F10a 17536795
Prothrombin Ki = 160.0 nM 6.8 Inhibition of human F2a 17536795

Literature References

PubMed DOI Target Context # Activities
17536795 10.1021/jm070125f Coagulation factor X 1
17536795 10.1021/jm070125f Prothrombin 1
17536795 10.1021/jm070125f Plasma 1
17536795 10.1021/jm070125f Unchecked 1

Data from ChEMBL 36 via Core Engine