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Compound Detail

CHEMBL104157

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N=C(N)c1cccc(C[C@H](NS(=O)(=O)c2ccc3ccccc3c2)C(=O)N2CCN(CCO)CC2)c1

Basic Information

ChEMBL ID CHEMBL104157
Phase Preclinical
Structure Type MOL
InChI Key SVQXGJDWUSQUPO-DEOSSOPVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

509.6
MW (Da)
1.15
ALogP
6
HBA
4
HBD
139.8
PSA (Ų)
0.25
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 C26H31N5O4S
MW 509.63
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.13

Activity Summary

Ki 2 meas. best 5.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 5.25 5.25 5600.0 1
Trypsin II
CHEMBL4472
Ki 4.41 4.41 39000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 5600.0 nM 5.25 Inhibitory activity against thrombin 9301673
Trypsin II Ki = 39000.0 nM 4.41 Inhibitory activity against trypsin 9301673

Literature References

PubMed DOI Target Context # Activities
9301673 10.1021/jm960668h Prothrombin 1
9301673 10.1021/jm960668h Trypsin II 1

Data from ChEMBL 36 via Core Engine