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Compound Detail

CHEMBL70404

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Cc1ccc(C2=CN=C(CCC(=O)N3CCN(C(=O)N4C(=O)[C@H](CC5CCNCC5)[C@H]4C(=O)O)CC3)C2=O)cc1

Basic Information

ChEMBL ID CHEMBL70404
Phase Preclinical
Structure Type MOL
InChI Key PHUOJJOCYCBHRI-BWKNWUBXSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

549.6
MW (Da)
1.71
ALogP
7
HBA
2
HBD
139.7
PSA (Ų)
0.49
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35N5O6
MW 549.63
Aromatic Rings 1
Heavy Atoms 40
NP-Likeness 0.03

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase
CHEMBL2095193
IC50 8.3 8.3 5.0 1
Serine protease 1
CHEMBL3769
IC50 5.75 5.75 1800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase IC50 = 5.0 nM 8.3 Inhibitory activity against human tryptase 15081015
Serine protease 1 IC50 = 1800.0 nM 5.75 Inhibitory activity against bovine trypsin 15081015

Literature References

PubMed DOI Target Context # Activities
15081015 10.1016/j.bmcl.2004.02.012 Tryptase 1
15081015 10.1016/j.bmcl.2004.02.012 Serine protease 1 1
15081015 10.1016/j.bmcl.2004.02.012 Unchecked 1

Data from ChEMBL 36 via Core Engine