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Compound Detail

CHEMBL210055

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COc1ccc(CCOc2ccc(Cc3nc(C(=O)[C@H](CCCCN)NC(=O)OCc4ccccc4)no3)cc2)cc1OC

Basic Information

ChEMBL ID CHEMBL210055
Phase Preclinical
Structure Type MOL
InChI Key NBEYVJNUMLSUGN-MHZLTWQESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

602.7
MW (Da)
4.91
ALogP
10
HBA
2
HBD
148.0
PSA (Ų)
0.13
QED
1
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H38N4O7
MW 602.69
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.41

Activity Summary

Ki 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.96 7.96 11.0 1
Tryptase beta-1
CHEMBL2617
Ki 7.62 7.62 24.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 11.0 nM 7.96 Binding affinity to trypsin 16725321
Tryptase beta-1 Ki = 24.0 nM 7.62 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