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Compound Detail

CHEMBL145664

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CN(C)c1cccc2c(S(=O)(=O)N[C@@H](Cc3cccc(C(=N)N)c3)C(=O)N3CCN(S(C)(=O)=O)CC3)cccc12

Basic Information

ChEMBL ID CHEMBL145664
Phase Preclinical
Structure Type MOL
InChI Key MOQBPFLLJRPCEX-QHCPKHFHSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

586.7
MW (Da)
1.18
ALogP
7
HBA
3
HBD
157.0
PSA (Ų)
0.25
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 C27H34N6O5S2
MW 586.74
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.28

Activity Summary

Ki 3 meas. best 8.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 8.38 8.38 4.2 1
Serine protease 1
CHEMBL3769
Ki 6.77 6.77 169.8 1
Coagulation factor X
CHEMBL244
Ki 5.41 5.41 3890.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 4.169 nM 8.38 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 169.82 nM 6.77 Binding affinity towards trypsin 9986717
Coagulation factor X Ki = 3890.45 nM 5.41 Binding affinity towards Coagulation factor Xa 9986717

Literature References

PubMed DOI Target Context # Activities
9986717 10.1021/jm981062r Prothrombin 1
9986717 10.1021/jm981062r Serine protease 1 1
9986717 10.1021/jm981062r Coagulation factor X 1

Data from ChEMBL 36 via Core Engine