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Compound Detail

CHEMBL557987

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COC(=O)N[C@@H](CCCCN)C(=O)c1noc(Cc2ccc(OCCc3ccc(Cl)c(Cl)c3)cc2)n1.Cl

Basic Information

ChEMBL ID CHEMBL557987
Phase Preclinical
Structure Type MOL
InChI Key WEQQZZSCJRBHQM-BOXHHOBZSA-N
Parent Compound CHEMBL1196719
Active Moiety CHEMBL1196719
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

535.4
MW (Da)
4.63
ALogP
8
HBA
2
HBD
129.6
PSA (Ų)
0.24
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29Cl3N4O5
MW 571.89
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.72

Activity Summary

Ki 2 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.77 7.77 17.0 1
Trypsin
CHEMBL2095204
Ki 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 17.0 nM 7.77 Inhibition of human B tryptase 16644215
Trypsin Ki = 2200.0 nM 5.66 Inhibition of trypsin 16644215

Literature References

PubMed DOI Target Context # Activities
16644215 10.1016/j.bmcl.2006.04.013 Unchecked 1
16644215 10.1016/j.bmcl.2006.04.013 Trypsin 1
16644215 10.1016/j.bmcl.2006.04.013 Tryptase beta-1 1

Data from ChEMBL 36 via Core Engine