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Compound Detail

CHEMBL218594

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CC(C)C[C@H](NC(=O)NCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1)C(C)C

Basic Information

ChEMBL ID CHEMBL218594
Phase Preclinical
Structure Type BOTH
InChI Key RLDZHJFLIIOAIL-FKBYEOEOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

586.8
MW (Da)
2.13
ALogP
7
HBA
7
HBD
191.2
PSA (Ų)
0.07
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H42N8O4S
MW 586.76
Aromatic Rings 2
Heavy Atoms 41
NP-Likeness -0.46

Activity Summary

IC50 2 meas. best 6.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 6.87 6.87 136.0 1
Prothrombin
CHEMBL204
IC50 5.55 5.55 2800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 136.0 nM 6.87 Inhibition of factor 11a 17181160
Prothrombin IC50 = 2800.0 nM 5.55 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