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Compound Detail

CHEMBL270206

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CCOC(=O)c1csc(C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC)n1

Basic Information

ChEMBL ID CHEMBL270206
Phase Preclinical
Structure Type BOTH
InChI Key LPKAGHKXANUXHY-ZVDOUQERSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

571.7
MW (Da)
1.07
ALogP
9
HBA
5
HBD
179.6
PSA (Ų)
0.07
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H37N7O5S
MW 571.70
Aromatic Rings 2
Heavy Atoms 40
NP-Likeness -0.44

Activity Summary

Ki 2 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.35 8.35 4.5 1
Unchecked
CHEMBL612545
Ki 8.27 8.27 5.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 4.5 nM 8.35 Inhibition of human alpha-thrombin 18053726
Unchecked Ki = 5.4 nM 8.27 Inhibition of bovine 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 Unchecked 1

Data from ChEMBL 36 via Core Engine