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Compound Detail

CHEMBL507020

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CC(C)CNC(=O)c1ccc(-c2ccc(-c3cscc3CN)cc2C(=O)Nc2ccc(C(=N)N)cc2)c(C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL507020
Phase Preclinical
Structure Type MOL
InChI Key NRTPJMXYAMIJHJ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

569.7
MW (Da)
5.16
ALogP
6
HBA
6
HBD
171.4
PSA (Ų)
0.11
QED
3
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N5O4S
MW 569.69
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.56

Activity Summary

IC50 5 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 11.0 11.0 0.0 1
Coagulation factor VII/tissue factor
CHEMBL2095194
IC50 10.48 10.48 0.0 1
Plasminogen
CHEMBL1801
IC50 9.64 9.64 0.2 1
Unchecked
CHEMBL612545
IC50 8.75 8.75 1.8 1
Prothrombin
CHEMBL204
IC50 6.96 6.96 110.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.01 nM 11.0 Inhibition of factor 10a 19409795
Coagulation factor VII/tissue factor IC50 = 0.033 nM 10.48 Inhibition of tissue factor/factor 7a 19409795
Plasminogen IC50 = 0.229 nM 9.64 Inhibition of plasmin 19409795
Unchecked IC50 = 1.77 nM 8.75 Inhibition of trypsin 19409795
Prothrombin IC50 = 110.48 nM 6.96 Inhibition of thrombin 19409795

Literature References

PubMed DOI Target Context # Activities
19409795 10.1016/j.bmc.2009.04.013 Unchecked 5
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor X 1
19409795 10.1016/j.bmc.2009.04.013 Coagulation factor VII/tissue factor 1
19409795 10.1016/j.bmc.2009.04.013 Plasminogen 1
19409795 10.1016/j.bmc.2009.04.013 Prothrombin 1

Data from ChEMBL 36 via Core Engine