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Compound Detail

CHEMBL213780

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NCCCC[C@H](NC(=O)OCc1ccccc1)C(=O)c1noc(Cc2ccc(C(=O)NCCc3ccccc3)cc2)n1

Basic Information

ChEMBL ID CHEMBL213780
Phase Preclinical
Structure Type MOL
InChI Key ZAXACLDYKLBPPT-MHZLTWQESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

569.7
MW (Da)
4.24
ALogP
8
HBA
3
HBD
149.4
PSA (Ų)
0.14
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 C32H35N5O5
MW 569.66
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.60

Activity Summary

Ki 2 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 8.49 8.49 3.2 1
Trypsin
CHEMBL2095204
Ki 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 3.2 nM 8.49 Inhibition of human beta tryptase 16714109
Trypsin Ki = 20.0 nM 7.7 Inhibition of human trypsin 16714109

Literature References

PubMed DOI Target Context # Activities
16714109 10.1016/j.bmcl.2006.05.009 Unchecked 1
16714109 10.1016/j.bmcl.2006.05.009 No relevant target 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