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Compound Detail

CHEMBL219440

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CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NNC(=O)NCc1ccc(Cl)c(Cl)c1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL219440
Phase Preclinical
Structure Type MOL
InChI Key QDPLYGJRLOCVME-SDHOMARFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

704.7
MW (Da)
3.14
ALogP
8
HBA
8
HBD
203.2
PSA (Ų)
0.03
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H39Cl2N9O4S
MW 704.69
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -0.66

Activity Summary

IC50 3 meas. best 7.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 7.03 7.03 93.0 1
Prothrombin
CHEMBL204
IC50 5.17 5.17 6700.0 1
Coagulation factor X
CHEMBL244
IC50 4.85 4.85 14200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 93.0 nM 7.03 Inhibition of factor 11a 17181160
Prothrombin IC50 = 6700.0 nM 5.17 Inhibition of thrombin 17181160
Coagulation factor X IC50 = 14200.0 nM 4.85 Inhibition of factor 10a 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