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Compound Detail

CHEMBL256027

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Cn1nnnc1C(=O)[C@@H](NC(=O)[C@@H]1CC[C@H]2CN(S(=O)(=O)Cc3ccccc3)CC(=O)N21)[C@H]1CC[C@H](N)CC1

Basic Information

ChEMBL ID CHEMBL256027
Phase Preclinical
Structure Type MOL
InChI Key DFDTTXLYOCLPSE-HVAMYJMISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

558.7
MW (Da)
-0.40
ALogP
10
HBA
2
HBD
173.5
PSA (Ų)
0.41
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 C25H34N8O5S
MW 558.67
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -1.23

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.3 8.3 5.0 1
Trypsin
CHEMBL2095204
Ki 4.46 4.46 35000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 5.0 nM 8.3 Inhibition of human alpha-thrombin 18053726
Trypsin Ki = 35000.0 nM 4.46 Inhibition of human trypsin 18053726

Literature References

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

Data from ChEMBL 36 via Core Engine