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Compound Detail

CHEMBL284549

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N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCN2CC[C@@](N)(Cc3ccccc3)C(=O)N12)C(=O)C(=O)NCCc1ccccc1

Basic Information

ChEMBL ID CHEMBL284549
Phase Preclinical
Structure Type MOL
InChI Key TWEWLGCOQPUDAQ-FOUYOVOOSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

576.7
MW (Da)
-0.18
ALogP
7
HBA
6
HBD
186.7
PSA (Ų)
0.08
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H40N8O4
MW 576.70
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness 0.01

Activity Summary

Ki 2 meas. best 10.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.15 10.15 0.1 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.071 nM 10.15 Binding affinity towards thrombin was determined 10212123
Prothrombin Ki = 0.071 nM 10.15 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
10212123 10.1021/jm980052n Prothrombin 2
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1

Data from ChEMBL 36 via Core Engine