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Compound Detail

CHEMBL402150

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CC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL402150
Phase Preclinical
Structure Type MOL
InChI Key ZEDMSBVBKUUZHF-GJZGRUSLSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
1.03
ALogP
6
HBA
3
HBD
143.8
PSA (Ų)
0.25
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H26N6O3S
MW 430.53
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.62

Activity Summary

Ki 2 meas. best 8.4
IC50 1 meas. best 4.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.4 8.06 4.0 2
Prothrombin
CHEMBL204
IC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 4.0 nM 8.4 Inhibition of bovine trypsin 18053726
Unchecked Ki = 19.0 nM 7.72 Inhibition of human beta-tryptase 18053726
Prothrombin IC50 = 14000.0 nM 4.85 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Unchecked 2
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1

Data from ChEMBL 36 via Core Engine