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Compound Detail

CHEMBL376806

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CNc1ccc(-c2ccc(C(=O)N[C@@H](CC(C)C)C(=O)O)cc2C(=O)O)c(C(=O)Nc2cccc(C(N)=O)c2)c1

Basic Information

ChEMBL ID CHEMBL376806
Phase Preclinical
Structure Type MOL
InChI Key QVARAJPOKUXDSA-DEOSSOPVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

546.6
MW (Da)
3.67
ALogP
6
HBA
6
HBD
187.9
PSA (Ų)
0.21
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30N4O7
MW 546.58
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.65

Activity Summary

IC50 1 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tissue factor
CHEMBL4081
IC50 6.82 6.82 150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tissue factor IC50 = 150.0 nM 6.82 Inhibition of human TF/FVIIa complex by chromogenic assay 17064913

Literature References

PubMed DOI Target Context # Activities
17064913 10.1016/j.bmc.2006.09.071 Plasma 2
17064913 10.1016/j.bmc.2006.09.071 Tissue factor 1
17064913 10.1016/j.bmc.2006.09.071 Coagulation factor X 1
17064913 10.1016/j.bmc.2006.09.071 Prothrombin 1
17064913 10.1016/j.bmc.2006.09.071 Trypsin 1

Data from ChEMBL 36 via Core Engine