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Compound Detail

CHEMBL28365

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N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCN2CC[C@@](N)(Cc3ccccc3)CN12)C(=O)C(=O)NCc1ccccc1

Basic Information

ChEMBL ID CHEMBL28365
Phase Preclinical
Structure Type MOL
InChI Key YZSIAGKEGXROBU-NDIVSWGXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

548.7
MW (Da)
0.26
ALogP
7
HBA
6
HBD
169.7
PSA (Ų)
0.09
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H40N8O3
MW 548.69
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -0.10

Activity Summary

Ki 2 meas. best 10.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.14 10.14 0.1 1
Serine protease 1
CHEMBL3769
Ki 10.14 10.14 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.073 nM 10.14 Inhibitory concentration against thrombin. 10212122
Serine protease 1 Ki = 0.073 nM 10.14 Inhibitory concentration against trypsin. 10212122

Literature References

PubMed DOI Target Context # Activities
10212122 10.1021/jm980354p Prothrombin 2
10212122 10.1021/jm980354p Serine protease 1 1

Data from ChEMBL 36 via Core Engine