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Compound Detail

CHEMBL536973

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Cl.NCCCC[C@H](NC(=O)C1CCOC1)C(=O)c1noc(Cc2ccc(OCCc3ccc(Cl)c(Cl)c3)cc2)n1

Basic Information

ChEMBL ID CHEMBL536973
Phase Preclinical
Structure Type MOL
InChI Key BUUXAQWQUYBIEB-ZAXUKBGBSA-N
Parent Compound CHEMBL1188644
Active Moiety CHEMBL1188644
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

575.5
MW (Da)
4.42
ALogP
8
HBA
2
HBD
129.6
PSA (Ų)
0.21
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33Cl3N4O5
MW 611.95
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.62

Activity Summary

Ki 2 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.66 7.66 22.0 1
Trypsin
CHEMBL2095204
Ki 5.96 5.96 1100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 22.0 nM 7.66 Inhibition of human B tryptase 16644215
Trypsin Ki = 1100.0 nM 5.96 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