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Compound Detail

CHEMBL362874

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NCc1cccc(C2CCN(C(=O)c3cc(C(N)=O)cc(-c4nc(-c5cccs5)no4)c3)CC2)c1

Basic Information

ChEMBL ID CHEMBL362874
Phase Preclinical
Structure Type MOL
InChI Key LPBADDHUZIZZHC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

487.6
MW (Da)
4.04
ALogP
7
HBA
2
HBD
128.3
PSA (Ų)
0.42
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25N5O3S
MW 487.59
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.64

Activity Summary

Ki 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptase beta-1
CHEMBL2617
Ki 8.82 8.82 1.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptase beta-1 Ki = 1.5 nM 8.82 Inhibitory activity against human mast cell tryptase beta 15546728

Literature References

PubMed DOI Target Context # Activities
15546728 10.1016/j.bmcl.2004.09.065 Tryptase beta-1 1
15546728 10.1016/j.bmcl.2004.09.065 Voltage-gated inwardly rectifying potassium channel KCNH2 1
15546728 10.1016/j.bmcl.2004.09.065 Cytochrome P450 2C9 1
15546728 10.1016/j.bmcl.2004.09.065 Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine