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Compound Detail

CHEMBL380012

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NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)c1noc(Cc2ccc(OCCc3ccc4ccccc4c3)cc2)n1

Basic Information

ChEMBL ID CHEMBL380012
Phase Preclinical
Structure Type MOL
InChI Key LHBQMECVQHKBKF-HKBQPEDESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

592.7
MW (Da)
6.04
ALogP
8
HBA
2
HBD
129.6
PSA (Ų)
0.11
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H36N4O5
MW 592.70
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -0.44

Activity Summary

Ki 2 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.57 7.57 27.0 1
Trypsin
CHEMBL2095204
Ki 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 27.0 nM 7.57 Binding affinity to human tryptase beta2 16725321
Trypsin Ki = 140.0 nM 6.85 Binding affinity to trypsin 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