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Compound Detail

CHEMBL265121

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

Basic Information

ChEMBL ID CHEMBL265121
Phase Preclinical
Structure Type MOL
InChI Key MGDHZAAGZWEIJU-CCMRYFRJSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

680.6
MW (Da)
1.28
ALogP
8
HBA
8
HBD
234.3
PSA (Ų)
0.06
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H38BrN9O5S
MW 680.63
Aromatic Rings 2
Heavy Atoms 43
NP-Likeness -0.47

Activity Summary

IC50 4 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 8.1 8.1 8.0 1
Plasma
CHEMBL613652
IC50 8.1 8.1 8.0 1
Prothrombin
CHEMBL204
IC50 6.4 6.4 400.0 1
Coagulation factor X
CHEMBL244
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 8.0 nM 8.1 Inhibition of factor 11a 17181160
Plasma IC50 = 8.0 nM 8.1 Anticoagulant activity in human plasma 17181160
Prothrombin IC50 = 400.0 nM 6.4 Inhibition of thrombin 17181160
Coagulation factor X IC50 = 1600.0 nM 5.8 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