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Compound Detail

CHEMBL137311

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

Basic Information

ChEMBL ID CHEMBL137311
Phase Preclinical
Structure Type MOL
InChI Key XUBBHZIMNINHAR-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
0.79
ALogP
7
HBA
6
HBD
175.3
PSA (Ų)
0.12
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N5O5S2
MW 491.60
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.71

Activity Summary

Ki 6 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 6.35 6.35 450.0 1
Coagulation factor X
CHEMBL3656
Ki 5.38 5.38 4200.0 1
Coagulation factor X
CHEMBL244
Ki 5.15 5.15 7100.0 1
Trypsin II
CHEMBL4472
Ki 4.72 4.72 19000.0 1
Plasma kallikrein
CHEMBL2000
Ki 4.54 4.54 29000.0 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