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Compound Detail

CHEMBL357660

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COC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](Cc1cccc(C(=N)N)c1)NS(=O)(=O)c1ccc2ccccc2c1

Basic Information

ChEMBL ID CHEMBL357660
Phase Preclinical
Structure Type MOL
InChI Key JJLGAHCDPYFKAX-AYCKEJKLSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

536.6
MW (Da)
2.81
ALogP
6
HBA
3
HBD
142.7
PSA (Ų)
0.23
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 C28H32N4O5S
MW 536.65
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.59

Activity Summary

Ki 3 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 7.02 7.02 95.9 1
Serine protease 1
CHEMBL3769
Ki 5.66 5.66 2197.9 1
Coagulation factor X
CHEMBL244
Ki 4.24 4.24 57942.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 95.94 nM 7.02 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 2197.86 nM 5.66 Binding affinity towards trypsin 9986717
Coagulation factor X Ki = 57942.87 nM 4.24 Binding affinity towards Coagulation factor Xa 9986717

Literature References

PubMed DOI Target Context # Activities
9986717 10.1021/jm981062r Prothrombin 1
9986717 10.1021/jm981062r Serine protease 1 1
9986717 10.1021/jm981062r Coagulation factor X 1

Data from ChEMBL 36 via Core Engine