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Compound Detail

CHEMBL127773

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CC(=O)N1CC(=O)C[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)c1nc2ccccc2s1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL127773
Phase Preclinical
Structure Type MOL
InChI Key SCXOSOADHOSUPT-YYLIZZNMSA-N
Parent Compound CHEMBL1180487
Active Moiety CHEMBL1180487
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

444.5
MW (Da)
0.21
ALogP
7
HBA
3
HBD
160.8
PSA (Ų)
0.23
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 C22H25F3N6O6S
MW 558.54
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.34

Activity Summary

Ki 2 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL209
Ki 8.0 8.0 9.9 1
Tryptase beta-1
CHEMBL2617
Ki 7.14 7.14 73.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 9.9 nM 8.0 In vitro inhibition of bovine trypsin. 12930148
Tryptase beta-1 Ki = 73.0 nM 7.14 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