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Compound Detail

CHEMBL340547

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N=C(N)NCCCC(NC(=O)C1CCCC1)C(=O)c1nc2ccccc2s1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL340547
Phase Preclinical
Structure Type MOL
InChI Key GTYDMDUUUJTBSW-UHFFFAOYSA-N
Parent Compound CHEMBL360684
Active Moiety CHEMBL360684
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
2.42
ALogP
5
HBA
4
HBD
121.0
PSA (Ų)
0.24
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H26F3N5O4S
MW 501.53
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.96

Activity Summary

Ki 2 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
Ki 7.52 7.52 30.0 1
Tryptase beta-1
CHEMBL2617
Ki 7.06 7.06 88.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 30.0 nM 7.52 In vitro inhibition of bovine trypsin. 12930148
Tryptase beta-1 Ki = 88.0 nM 7.06 In vitro inhibition of human Tryptase beta. 12930148

Literature References

PubMed DOI Target Context # Activities
12930148 10.1021/jm030050p Tryptase beta-1 1
12930148 10.1021/jm030050p Serine protease 1 1

Data from ChEMBL 36 via Core Engine