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Compound Detail

CHEMBL263252

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)Nc3ccc(-c4ccccc4C[n+]4ccccc4)cc3F)cc12.[Br-]

Basic Information

ChEMBL ID CHEMBL263252
Phase Preclinical
Structure Type MOL
InChI Key BGBZSDBCADGKAD-UHFFFAOYSA-N
Parent Compound CHEMBL1182732
Active Moiety CHEMBL1182732
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

573.5
MW (Da)
6.01
ALogP
6
HBA
2
HBD
102.8
PSA (Ų)
0.19
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H21BrF4N6O2
MW 653.43
Aromatic Rings 6
Heavy Atoms 42
NP-Likeness -1.42

Activity Summary

Ki 1 meas. best 10.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.1 10.1 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.08 nM 10.1 Binding affinity to human factor 10a 16434195

Literature References

PubMed DOI Target Context # Activities
16434195 10.1016/j.bmcl.2006.01.010 Coagulation factor X 1
16434195 10.1016/j.bmcl.2006.01.010 Caco-2 1
16434195 10.1016/j.bmcl.2006.01.010 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine