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Compound Detail

CHEMBL214368

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CCOC(=O)N[C@@H](CCCCN)C(=O)c1noc(Cc2ccc(C(=O)NC3Cc4ccccc4C3)cc2)n1

Basic Information

ChEMBL ID CHEMBL214368
Phase Preclinical
Structure Type MOL
InChI Key PWHBUXLKTXHYAP-QHCPKHFHSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

519.6
MW (Da)
2.98
ALogP
8
HBA
3
HBD
149.4
PSA (Ų)
0.24
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H33N5O5
MW 519.60
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.67

Activity Summary

Ki 5 meas. best 8.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 8.55 8.55 2.8 1
Unchecked
CHEMBL612545
Ki 8.52 8.52 3.0 1
Trypsin
CHEMBL2095204
Ki 6.77 6.77 170.0 1
Prothrombin
CHEMBL204
Ki 4.22 4.22 60000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 2.8 nM 8.55 Inhibition of human beta tryptase 16714109
Unchecked Ki = 3.0 nM 8.52 Inhibition of human beta-tryptase 18053726
Trypsin Ki = 170.0 nM 6.77 Inhibition of human trypsin 16714109
Prothrombin Ki = 60000.0 nM 4.22 Inhibition of thrombin 16714109

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Unchecked 4
16714109 10.1016/j.bmcl.2006.05.009 Liver microsomes 1
16714109 10.1016/j.bmcl.2006.05.009 Coagulation factor X 1
16714109 10.1016/j.bmcl.2006.05.009 Prothrombin 1
16714109 10.1016/j.bmcl.2006.05.009 Coagulation factor VII 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