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Compound Detail

CHEMBL1161253

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N=C(N)c1cccc(C[C@H](NS(=O)(=O)c2ccc3ccccc3c2)C(=O)N2CCCC[C@@H]2C(=O)O)c1

Basic Information

ChEMBL ID CHEMBL1161253
Phase Preclinical
Structure Type MOL
InChI Key GNANSBQAIRJZPA-XZOQPEGZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

508.6
MW (Da)
2.48
ALogP
5
HBA
4
HBD
153.7
PSA (Ų)
0.27
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C26H28N4O5S
MW 508.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.72

Activity Summary

Ki 3 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 6.58 6.58 260.0 1
Serine protease 1
CHEMBL3769
Ki 6.2 6.2 631.0 1
Coagulation factor X
CHEMBL244
Ki 4.42 4.42 38018.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 260.02 nM 6.58 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 630.96 nM 6.2 Binding affinity towards trypsin 9986717
Coagulation factor X Ki = 38018.94 nM 4.42 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