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Compound Detail

CHEMBL179910

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NC(N)=NCCCC(NC(=O)[C@@H]1CCCN1C(=O)[C@H](N)Cc1ccccc1)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL179910
Phase Preclinical
Structure Type MOL
InChI Key XZUXATAIZFXMEK-IZWFHCBGSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

535.7
MW (Da)
1.58
ALogP
7
HBA
4
HBD
169.8
PSA (Ų)
0.12
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N7O3S
MW 535.67
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.43

Activity Summary

IC50 1 meas. best 7.68
Ki 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 9.52 9.52 0.3 1
Prothrombin
CHEMBL204
IC50 7.68 7.68 21.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 0.3 nM 9.52 Binding affinity against bovine trypsin 15771442
Prothrombin IC50 = 21.0 nM 7.68 Inhibitory concentration against human alpha thrombin 15771442

Literature References

PubMed DOI Target Context # Activities
15771442 10.1021/jm0303857 Prothrombin 2
15771442 10.1021/jm0303857 Serine protease 1 1

Data from ChEMBL 36 via Core Engine