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Compound Detail

CHEMBL341933

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N=C(N)c1ccc(CC(NC(=O)CNS(=O)(=O)c2ccc(C(=N)N)cc2)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL341933
Phase Preclinical
Structure Type MOL
InChI Key MREBMJAXNFLJHN-UHFFFAOYSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

446.5
MW (Da)
-0.65
ALogP
6
HBA
7
HBD
212.3
PSA (Ų)
0.18
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H22N6O5S
MW 446.49
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.62

Activity Summary

Ki 6 meas. best 5.58
IC50 1 meas. best 4.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL3656
Ki 5.58 5.58 2600.0 1
Coagulation factor X
CHEMBL244
Ki 5.44 5.44 3600.0 1
Trypsin II
CHEMBL4472
Ki 4.75 4.75 18000.0 1
Plasma kallikrein
CHEMBL2000
Ki 4.72 4.72 19000.0 1
Plasminogen
CHEMBL1801
Ki 4.24 4.24 57000.0 1
Tryptase gamma
CHEMBL4955
IC50 4.19 4.19 65000.0 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