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Compound Detail

CHEMBL207981

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Cc1cc(CNC(=O)[C@@H]2C=CCN2C(=O)C(CC2CCCCC2)NCC(=O)O)sc1C(=N)N

Basic Information

ChEMBL ID CHEMBL207981
Phase Preclinical
Structure Type MOL
InChI Key GJKMIUMNDMWVGF-ZVAWYAOSSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
1.74
ALogP
6
HBA
5
HBD
148.6
PSA (Ų)
0.20
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H33N5O4S
MW 475.62
Aromatic Rings 1
Heavy Atoms 33
NP-Likeness -0.34

Activity Summary

IC50 3 meas. best 8.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 8.75 8.75 1.8 1
Trypsin
CHEMBL2095204
IC50 6.93 6.93 117.0 1
Tissue-type plasminogen activator
CHEMBL1873
IC50 6.16 6.16 687.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 1.76 nM 8.75 Inhibition of thrombin 16517159
Trypsin IC50 = 117.0 nM 6.93 Inhibition of trypsin 16517159
Tissue-type plasminogen activator IC50 = 687.0 nM 6.16 Inhibition of tPA 16517159

Literature References

PubMed DOI Target Context # Activities
16517159 10.1016/j.bmcl.2006.02.040 Rattus norvegicus 2
16517159 10.1016/j.bmcl.2006.02.040 Prothrombin 1
16517159 10.1016/j.bmcl.2006.02.040 Trypsin 1
16517159 10.1016/j.bmcl.2006.02.040 Tissue-type plasminogen activator 1
16517159 10.1016/j.bmcl.2006.02.040 Plasminogen 1
16517159 10.1016/j.bmcl.2006.02.040 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine