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Compound Detail

CHEMBL375816

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CC(C)[C@H](NC(=O)[C@@H](NC(=O)N[C@H](C)c1ccc(Br)cc1)C1CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL375816
Phase Preclinical
Structure Type MOL
InChI Key OLQGYESZUNMFCC-RYCFVGSHSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

705.7
MW (Da)
3.99
ALogP
7
HBA
7
HBD
191.2
PSA (Ų)
0.06
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H45BrN8O4S
MW 705.72
Aromatic Rings 2
Heavy Atoms 45
NP-Likeness -0.52

Activity Summary

IC50 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 8.0 8.0 10.0 1
Plasma
CHEMBL613652
IC50 8.0 8.0 10.0 1
Prothrombin
CHEMBL204
IC50 6.01 6.01 976.0 1
Coagulation factor X
CHEMBL244
IC50 5.57 5.57 2700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 10.0 nM 8.0 Inhibition of factor 11a 17181160
Plasma IC50 = 10.0 nM 8.0 Anticoagulant activity in human plasma 17181160
Prothrombin IC50 = 976.0 nM 6.01 Inhibition of thrombin 17181160
Coagulation factor X IC50 = 2700.0 nM 5.57 Inhibition of factor 10a 17181160

Literature References

PubMed DOI Target Context # Activities
17181160 10.1021/jm060978s Plasma 3
17181160 10.1021/jm060978s Coagulation factor XI 1
17181160 10.1021/jm060978s Coagulation factor X 1
17181160 10.1021/jm060978s Prothrombin 1

Data from ChEMBL 36 via Core Engine