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Compound Detail

CHEMBL143205

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CNC(=O)C1CCN(C(=O)[C@H](Cc2cccc(C(=N)N)c2)NS(=O)(=O)c2ccc3ccccc3c2)CC1

Basic Information

ChEMBL ID CHEMBL143205
Phase Preclinical
Structure Type MOL
InChI Key TYMQNVQSZHECHF-DEOSSOPVSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

521.6
MW (Da)
2.00
ALogP
5
HBA
4
HBD
145.4
PSA (Ų)
0.26
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 C27H31N5O4S
MW 521.64
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.19

Activity Summary

Ki 3 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 6.8 6.8 160.0 1
Prothrombin
CHEMBL4471
Ki 6.8 6.8 160.0 1
Coagulation factor X
CHEMBL244
Ki 4.12 4.12 76032.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 159.96 nM 6.8 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 159.96 nM 6.8 Binding affinity towards trypsin 9986717
Coagulation factor X Ki = 76032.63 nM 4.12 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