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Compound Detail

CHEMBL213698

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COc1ccc(Cc2nc(C(=O)[C@H](CCCCN)NC(=O)OCc3ccccc3)no2)cc1

Basic Information

ChEMBL ID CHEMBL213698
Phase Preclinical
Structure Type MOL
InChI Key BJXLDDFCVLFRRC-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

452.5
MW (Da)
3.28
ALogP
8
HBA
2
HBD
129.6
PSA (Ų)
0.32
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N4O5
MW 452.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.50

Activity Summary

Ki 2 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypsin
CHEMBL2095204
Ki 7.66 7.66 22.0 1
Tryptase beta-1
CHEMBL2617
Ki 6.11 6.11 770.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypsin Ki = 22.0 nM 7.66 Inhibition of human trypsin 16714109
Tryptase beta-1 Ki = 770.0 nM 6.11 Inhibition of human beta tryptase 16714109

Literature References

PubMed DOI Target Context # Activities
16714109 10.1016/j.bmcl.2006.05.009 Voltage-gated inwardly rectifying potassium channel KCNH2 1
16714109 10.1016/j.bmcl.2006.05.009 No relevant target 1
16714109 10.1016/j.bmcl.2006.05.009 Unchecked 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