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Compound Detail

CHEMBL83106

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COc1ccc(Oc2nc(Oc3cccc(C(=N)N)c3)c(F)c(C)c2F)cc1C(=O)N(C)C

Basic Information

ChEMBL ID CHEMBL83106
Phase Preclinical
Structure Type MOL
InChI Key GAEBEPXLMSRMNB-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

456.4
MW (Da)
4.25
ALogP
6
HBA
2
HBD
110.8
PSA (Ų)
0.41
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22F2N4O4
MW 456.45
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.01

Activity Summary

Ki 4 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 6.35 6.35 450.0 1
Coagulation factor X
CHEMBL244
Ki 5.85 5.85 1400.0 2
Prothrombin
CHEMBL204
Ki 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14667222 10.1021/jm030288d Coagulation factor X 1
12036356 10.1021/jm0200660 Coagulation factor X 1
12036356 10.1021/jm0200660 Prothrombin 1
12036356 10.1021/jm0200660 Serine protease 1 1

Data from ChEMBL 36 via Core Engine