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Compound Detail

CHEMBL209604

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NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)c1noc(CN2CCN(CCCc3ccccc3)CC2)n1

Basic Information

ChEMBL ID CHEMBL209604
Phase Preclinical
Structure Type MOL
InChI Key MWDTYWNRQRBAGQ-SANMLTNESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

548.7
MW (Da)
3.43
ALogP
9
HBA
2
HBD
126.8
PSA (Ų)
0.22
QED
1
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H40N6O4
MW 548.69
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.81

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 7.96 7.96 11.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 11.0 nM 7.96 Inhibition of human trypsin 16714109
Tryptase beta-1 Ki = 11.0 nM 7.96 Inhibition of human beta tryptase 16714109

Literature References

PubMed DOI Target Context # Activities
16714109 10.1016/j.bmcl.2006.05.009 No relevant target 1
16714109 10.1016/j.bmcl.2006.05.009 Liver microsomes 1
16714109 10.1016/j.bmcl.2006.05.009 Trypsin 1
16714109 10.1016/j.bmcl.2006.05.009 Tryptase beta-1 1

Data from ChEMBL 36 via Core Engine