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Compound Detail

CHEMBL215870

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CC(C)[C@@H](NCC(=O)O)C(=O)NC1(C(=O)NCc2ccc(C(=N)N)cc2)Cc2cccnc2C1

Basic Information

ChEMBL ID CHEMBL215870
Phase Preclinical
Structure Type MOL
InChI Key LYYIHOVBKSYKLS-CGHJUBPDSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

466.5
MW (Da)
0.33
ALogP
6
HBA
6
HBD
170.3
PSA (Ų)
0.22
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N6O4
MW 466.54
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -0.49

Activity Summary

IC50 4 meas. best 5.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vitamin K-dependent protein C
CHEMBL4444
IC50 5.97 5.955 1070.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Vitamin K-dependent protein C IC50 = 1070.0 nM 5.97 Inhibition of human aPC 16913694
Vitamin K-dependent protein C IC50 = 1140.0 nM 5.94 Inhibition of human aPC 16913694

Literature References

PubMed DOI Target Context # Activities
16913694 10.1021/jm0606950 Prothrombin 2
16913694 10.1021/jm0606950 Vitamin K-dependent protein C 2

Data from ChEMBL 36 via Core Engine