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Compound Detail

CHEMBL423195

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COc1cc(C)c(S(=O)(=O)N[C@@H](Cc2cccc(C(=N)N)c2)C(=O)N2CCN(S(C)(=O)=O)CC2)c(C)c1C

Basic Information

ChEMBL ID CHEMBL423195
Phase Preclinical
Structure Type MOL
InChI Key KIRQVCXFBXDMRQ-NRFANRHFSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
0.90
ALogP
7
HBA
3
HBD
163.0
PSA (Ų)
0.30
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35N5O6S2
MW 565.72
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.08

Activity Summary

Ki 3 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 7.5 7.5 32.0 1
Serine protease 1
CHEMBL3769
Ki 5.75 5.75 1798.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 31.99 nM 7.5 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 1798.87 nM 5.75 Binding affinity towards trypsin 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