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Compound Detail

CHEMBL595663

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CN1CCc2nc(C(=O)N[C@@H]3C[C@@H](C(=O)N(C)C)CC[C@@H]3NC(=O)c3cc4ccc(Cl)cc4nn3)sc2C1

Basic Information

ChEMBL ID CHEMBL595663
Phase Preclinical
Structure Type MOL
InChI Key PNQXOEXOFLZKCD-RIFZZMRRSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

556.1
MW (Da)
2.51
ALogP
8
HBA
2
HBD
120.4
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30ClN7O3S
MW 556.09
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.29

Activity Summary

IC50 1 meas. best 8.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.48 8.48 3.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.026 nmol/min/mg Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 3.3 nM 8.48 Inhibition of human factor 10a by microplate spectrophotometry 19900814

Literature References

PubMed DOI Target Context # Activities
19900814 10.1016/j.bmc.2009.10.024 No relevant target 3
19900814 10.1016/j.bmc.2009.10.024 Liver microsomes 1
19900814 10.1016/j.bmc.2009.10.024 Rattus norvegicus 1
19900814 10.1016/j.bmc.2009.10.024 Plasma 1
19900814 10.1016/j.bmc.2009.10.024 Coagulation factor X 1
19900814 10.1016/j.bmc.2009.10.024 Caco-2 1

Data from ChEMBL 36 via Core Engine