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Compound Detail

CHEMBL538085

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Cc1cc(C(=O)N[C@@H](CCCCN)C(=O)c2noc(Cc3ccc(OCCc4ccc(Cl)c(Cl)c4)cc3)n2)c(C)o1.Cl

Basic Information

ChEMBL ID CHEMBL538085
Phase Preclinical
Structure Type MOL
InChI Key TWOIRSMXFJVZBL-SNYZSRNZSA-N
Parent Compound CHEMBL1189135
Active Moiety CHEMBL1189135
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

599.5
MW (Da)
5.91
ALogP
8
HBA
2
HBD
133.5
PSA (Ų)
0.14
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33Cl3N4O5
MW 635.98
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.87

Activity Summary

Ki 2 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 7.34 7.34 46.0 1
Trypsin
CHEMBL2095204
Ki 5.41 5.41 3900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 46.0 nM 7.34 Inhibition of human B tryptase 16644215
Trypsin Ki = 3900.0 nM 5.41 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