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Compound Detail

CHEMBL502858

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Cc1ccc2oc(=O)c(C(=O)Nc3ccccc3C)cc2c1

Basic Information

ChEMBL ID CHEMBL502858
Phase Preclinical
Structure Type MOL
InChI Key FCSXWWMASMRVEL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

293.3
MW (Da)
3.66
ALogP
3
HBA
1
HBD
59.3
PSA (Ų)
0.73
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H15NO3
MW 293.32
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 4.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XII
CHEMBL2821
IC50 4.5 4.5 32000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XII IC50 = 32000.0 nM 4.5 Inhibition of human factor 12a 18459730

Literature References

PubMed DOI Target Context # Activities
18459730 10.1021/jm8002697 Coagulation factor X 1
18459730 10.1021/jm8002697 Coagulation factor VII/tissue factor 1
18459730 10.1021/jm8002697 Plasma kallikrein 1
18459730 10.1021/jm8002697 Coagulation factor XII 1
18459730 10.1021/jm8002697 Prothrombin 1

Data from ChEMBL 36 via Core Engine