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Compound Detail

CHEMBL135198

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CCOC(=O)C(Cc1ccc(C(=N)N)cc1)NC(=O)CNS(=O)(=O)c1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL135198
Phase Preclinical
Structure Type MOL
InChI Key CMUBVICFNAQVEP-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
0.41
ALogP
7
HBA
4
HBD
175.2
PSA (Ų)
0.23
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N5O5S
MW 457.51
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.12

Activity Summary

Ki 5 meas. best 5.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL3656
Ki 5.32 5.32 4800.0 1
Coagulation factor X
CHEMBL244
Ki 5.06 5.06 8700.0 1
Prothrombin
CHEMBL4471
Ki 4.96 4.96 11000.0 1
Plasma kallikrein
CHEMBL2000
Ki 4.75 4.75 18000.0 1
Trypsin II
CHEMBL4472
Ki 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9784099 10.1021/jm980227t Coagulation factor X 2
9784099 10.1021/jm980227t Prothrombin 1
9784099 10.1021/jm980227t Vitamin K-dependent protein C 1
9784099 10.1021/jm980227t Plasma kallikrein 1
9784099 10.1021/jm980227t Plasminogen 1
9784099 10.1021/jm980227t Urokinase-type plasminogen activator 1
9784099 10.1021/jm980227t Unchecked 1
9784099 10.1021/jm980227t Trypsin II 1
9784099 10.1021/jm980227t Tryptase gamma 1

Data from ChEMBL 36 via Core Engine