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Compound Detail

CHEMBL341083

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CC(=O)N1C[C@H](O)C[C@H]1C(=O)NC(CCCN=C(N)N)C(=O)c1nccs1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL341083
Phase Preclinical
Structure Type MOL
InChI Key SKAYCANUSOVOCT-QRVSAPIOSA-N
Parent Compound CHEMBL1184248
Active Moiety CHEMBL1184248
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

396.5
MW (Da)
-1.15
ALogP
7
HBA
4
HBD
164.0
PSA (Ų)
0.19
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 C18H25F3N6O6S
MW 510.50
Aromatic Rings 1
Heavy Atoms 27
NP-Likeness 0.10

Activity Summary

Ki 2 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
Ki 7.09 7.09 81.0 1
Tryptase beta-1
CHEMBL2617
Ki 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 81.0 nM 7.09 In vitro inhibition of bovine trypsin. 12930148
Tryptase beta-1 Ki = 180.0 nM 6.75 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