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Compound Detail

CHEMBL143067

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COc1cc(C)c(S(=O)(=O)N[C@@H](Cc2cccc(C(=N)N)c2)C(=O)N2CCC(C)CC2)c(C)c1C

Basic Information

ChEMBL ID CHEMBL143067
Phase Preclinical
Structure Type MOL
InChI Key XASLMEPRPDINAK-QFIPXVFZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

500.7
MW (Da)
3.05
ALogP
5
HBA
3
HBD
125.6
PSA (Ų)
0.38
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H36N4O4S
MW 500.67
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.84

Activity Summary

Ki 3 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL4471
Ki 7.05 7.05 88.9 1
Serine protease 1
CHEMBL3769
Ki 6.11 6.11 779.8 1
Coagulation factor X
CHEMBL244
Ki 4.0 4.0 100000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 88.92 nM 7.05 Binding affinity towards thrombin 9986717
Serine protease 1 Ki = 779.83 nM 6.11 Binding affinity towards trypsin 9986717
Coagulation factor X Ki = 100000.0 nM 4.0 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