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Compound Detail

CHEMBL431557

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O=C(O)[C@@H]1[C@@H](CC2CCNCC2)C(=O)N1C(=O)N1CCN(C(=O)c2ccc(Oc3ccccc3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL431557
Phase Preclinical
Structure Type MOL
InChI Key AUYOZPJOPWTGLF-RPWUZVMVSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
2.66
ALogP
6
HBA
2
HBD
119.5
PSA (Ų)
0.56
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N4O6
MW 520.59
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.29

Activity Summary

IC50 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
IC50 8.15 8.15 7.0 1
Serine protease 1
CHEMBL3769
IC50 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase IC50 = 7.0 nM 8.15 Inhibitory activity against human tryptase 15081015
Serine protease 1 IC50 = 140.0 nM 6.85 Inhibitory activity against bovine trypsin 15081015

Literature References

PubMed DOI Target Context # Activities
15081015 10.1016/j.bmcl.2004.02.012 Tryptase 1
15081015 10.1016/j.bmcl.2004.02.012 Serine protease 1 1
15081015 10.1016/j.bmcl.2004.02.012 Unchecked 1

Data from ChEMBL 36 via Core Engine