Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL402109

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CN(C)Cc1nccn1-c1ccc(N2CC[C@H](NS(=O)(=O)/C=C/c3ccc(Cl)s3)C2=O)c(F)c1

Basic Information

ChEMBL ID CHEMBL402109
Phase Preclinical
Structure Type MOL
InChI Key KJUQWLSBEXCOOD-HCWHUNCVSA-N
1
Targets
2
Activities
1
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

524.0
MW (Da)
3.48
ALogP
7
HBA
1
HBD
87.5
PSA (Ų)
0.49
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23ClFN5O3S2
MW 524.04
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -2.08

Activity Summary

Ki 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.7 9.7 0.2 2

Pharmacokinetic Data

Parameter Value Units Species
CL 13.0 mL.min-1.kg-1 Rattus norvegicus
F 52.0 % Rattus norvegicus
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.2 nM 9.7 Inhibition of human factor 10a by fluorescence assay 20006499
Coagulation factor X Ki = 0.2 nM 9.7 Inhibition of factor 10a 20503967

Literature References

PubMed DOI Target Context # Activities
20503967 10.1021/jm100146h Rattus norvegicus 4
18053714 10.1016/j.bmcl.2007.11.019 Coagulation factor X 1
18053714 10.1016/j.bmcl.2007.11.019 Unchecked 1
20006499 10.1016/j.bmcl.2009.11.077 Plasma 1
20006499 10.1016/j.bmcl.2009.11.077 Coagulation factor X 1
20503967 10.1021/jm100146h Coagulation factor X 1
20503967 10.1021/jm100146h NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine