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Compound Detail

CHEMBL356153

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CCOC(=O)CS(=O)(=O)N(Cc1ccc2ccc(C(=N)N)cc2c1)c1ccc(OC2CCN(C(C)=N)CC2)cc1

Basic Information

ChEMBL ID CHEMBL356153
Phase Preclinical
Structure Type MOL
InChI Key CSHXIHWIECFVRC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
3.86
ALogP
7
HBA
3
HBD
149.9
PSA (Ų)
0.19
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 C29H35N5O5S
MW 565.70
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.68

Activity Summary

IC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 8.22 8.22 6.0 1
Trypsin II
CHEMBL4290
IC50 7.08 7.08 83.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 6.0 nM 8.22 Inhibitory concentration to factor Xa 12565972
Trypsin II IC50 = 83.0 nM 7.08 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 Trypsin II 1
12565972 10.1016/s0960-894x(02)00927-7 Unchecked 1

Data from ChEMBL 36 via Core Engine