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Compound Detail

CHEMBL256253

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N=C(N)NCCC[C@H](NC(=O)[C@@H]1CC[C@H]2CN(S(=O)(=O)Cc3ccccc3)CC(=O)N21)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL256253
Phase Preclinical
Structure Type MOL
InChI Key YDGHLKGMRRJCDM-FHWLQOOXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

561.7
MW (Da)
0.28
ALogP
8
HBA
4
HBD
178.7
PSA (Ų)
0.13
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H31N7O5S2
MW 561.69
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.79

Activity Summary

Ki 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.7 9.7 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.2 nM 9.7 Inhibition of human alpha-thrombin 18053726

Literature References

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

Data from ChEMBL 36 via Core Engine