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Compound Detail

CHEMBL265598

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

Basic Information

ChEMBL ID CHEMBL265598
Phase Preclinical
Structure Type BOTH
InChI Key QKIKHWOCEVLRKJ-QNWVGRARSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

669.7
MW (Da)
3.83
ALogP
7
HBA
7
HBD
191.2
PSA (Ų)
0.06
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H42Cl2N8O4S
MW 669.68
Aromatic Rings 2
Heavy Atoms 44
NP-Likeness -0.36

Activity Summary

IC50 2 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 5.04 5.04 9200.0 1
Prothrombin
CHEMBL204
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 9200.0 nM 5.04 Inhibition of factor 11a 17181160
Prothrombin IC50 = 12000.0 nM 4.92 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