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Compound Detail

CHEMBL493601

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O=C(Nc1ccccc1)c1cc2cc(Cl)cc(Br)c2oc1=O

Basic Information

ChEMBL ID CHEMBL493601
Phase Preclinical
Structure Type MOL
InChI Key IUBMSLQOIUSAFA-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

378.6
MW (Da)
4.46
ALogP
3
HBA
1
HBD
59.3
PSA (Ų)
0.67
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 C16H9BrClNO3
MW 378.61
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.30

Activity Summary

IC50 2 meas. best 5.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XII
CHEMBL2821
IC50 5.36 5.08 4400.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18459730 10.1021/jm8002697 Coagulation factor XII 2
26827162 10.1016/j.ejmech.2016.01.023 Coagulation factor XII 2
18459730 10.1021/jm8002697 Prothrombin 1
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
26827162 10.1016/j.ejmech.2016.01.023 Prothrombin 1
26827162 10.1016/j.ejmech.2016.01.023 Coagulation factor X 1
26827162 10.1016/j.ejmech.2016.01.023 Plasma kallikrein 1
26827162 10.1016/j.ejmech.2016.01.023 Coagulation factor VII 1
26827162 10.1016/j.ejmech.2016.01.023 No relevant target 1

Data from ChEMBL 36 via Core Engine