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Compound Detail

CHEMBL153134

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CC(=N)N1CCC(Oc2ccc(N(Cc3cc4ccc(C(=N)N)cc4n3C)S(C)(=O)=O)cc2)CC1

Basic Information

ChEMBL ID CHEMBL153134
Phase Preclinical
Structure Type MOL
InChI Key UCJLZYHARBIVAX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

496.6
MW (Da)
3.27
ALogP
6
HBA
3
HBD
128.5
PSA (Ų)
0.34
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32N6O3S
MW 496.64
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 9.1 9.1 0.8 1
Trypsin II
CHEMBL4290
IC50 7.6 7.6 25.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.8 nM 9.1 Inhibitory concentration to factor Xa 12565972
Trypsin II IC50 = 25.0 nM 7.6 Inhibitory concentration against trypsin 12565972

Literature References

PubMed DOI Target Context # Activities
12565972 10.1016/s0960-894x(02)00927-7 Coagulation factor X 1
12565972 10.1016/s0960-894x(02)00927-7 Prothrombin 1
12565972 10.1016/s0960-894x(02)00927-7 Trypsin II 1
12565972 10.1016/s0960-894x(02)00927-7 Unchecked 1

Data from ChEMBL 36 via Core Engine