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Compound Detail

CHEMBL214315

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NCCC[C@H](NC(=O)OCc1ccccc1)C(=O)c1noc(Cc2ccccc2)n1

Basic Information

ChEMBL ID CHEMBL214315
Phase Preclinical
Structure Type MOL
InChI Key XKLNZLFHJUGPKG-SFHVURJKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
2.88
ALogP
7
HBA
2
HBD
120.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24N4O4
MW 408.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.50

Activity Summary

Ki 2 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.17 7.17 68.0 1
Tryptase beta-1
CHEMBL2617
Ki 5.57 5.57 2700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 68.0 nM 7.17 Binding affinity to trypsin 16725321
Tryptase beta-1 Ki = 2700.0 nM 5.57 Binding affinity to human tryptase beta2 16725321

Literature References

PubMed DOI Target Context # Activities
16725321 10.1016/j.bmcl.2006.04.088 Trypsin 2
16725321 10.1016/j.bmcl.2006.04.088 Tryptase beta-1 1

Data from ChEMBL 36 via Core Engine