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Compound Detail

CHEMBL384971

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

Basic Information

ChEMBL ID CHEMBL384971
Phase Preclinical
Structure Type MOL
InChI Key WBAKUPSUHRKONA-MNAPGUCWSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

722.7
MW (Da)
1.67
ALogP
8
HBA
10
HBD
253.1
PSA (Ų)
0.05
QED
2
Ro5 Violations
18
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H44BrN11O4S
MW 722.71
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.51

Activity Summary

IC50 3 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 8.15 8.15 7.0 1
Coagulation factor X
CHEMBL244
IC50 6.6 6.6 250.0 1
Prothrombin
CHEMBL204
IC50 6.36 6.36 440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 7.0 nM 8.15 Inhibition of factor 11a 17181160
Coagulation factor X IC50 = 250.0 nM 6.6 Inhibition of factor 10a 17181160
Prothrombin IC50 = 440.0 nM 6.36 Inhibition of thrombin 17181160

Literature References

PubMed DOI Target Context # Activities
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