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Compound Detail

CHEMBL105439

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COc1cc(C)c(S(=O)(=O)NC(Cc2cccc(C(=N)N)c2)C(=O)N2CCN(S(C)(=O)=O)CC2)c(C)c1C

Basic Information

ChEMBL ID CHEMBL105439
Phase Preclinical
Structure Type MOL
InChI Key KIRQVCXFBXDMRQ-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
0.90
ALogP
7
HBA
3
HBD
163.0
PSA (Ų)
0.30
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H35N5O6S2
MW 565.72
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.08

Activity Summary

Ki 4 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 7.5 7.5 32.0 1
Trypsin II
CHEMBL4472
Ki 5.75 5.75 1800.0 1
Plasminogen
CHEMBL1801
Ki 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 32.0 nM 7.5 Inhibitory activity against thrombin 9301673
Trypsin II Ki = 1800.0 nM 5.75 Inhibitory activity against trypsin 9301673
Plasminogen Ki = 18000.0 nM 4.75 Inhibitory activity against plasmin 9301673

Literature References

PubMed DOI Target Context # Activities
9301673 10.1021/jm960668h Prothrombin 1
9301673 10.1021/jm960668h Coagulation factor X 1
9301673 10.1021/jm960668h Plasminogen 1
9301673 10.1021/jm960668h Trypsin II 1

Data from ChEMBL 36 via Core Engine