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Compound Detail

CHEMBL266570

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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

Basic Information

ChEMBL ID CHEMBL266570
Phase Preclinical
Structure Type BOTH
InChI Key TZODCMWFXOTDNK-FKBYEOEOSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

655.6
MW (Da)
3.44
ALogP
7
HBA
7
HBD
191.2
PSA (Ų)
0.06
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 C28H40Cl2N8O4S
MW 655.65
Aromatic Rings 2
Heavy Atoms 43
NP-Likeness -0.62

Activity Summary

IC50 4 meas. best 7.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 7.2 7.2 63.0 2
Prothrombin
CHEMBL204
IC50 6.06 5.82 876.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 63.0 nM 7.2 Inhibition of factor 11a 17181160
Coagulation factor XI IC50 = 63.0 nM 7.2 Inhibition of human factor 11a 18053726
Prothrombin IC50 = 876.0 nM 6.06 Inhibition of thrombin 17181160
Prothrombin IC50 = 2600.0 nM 5.58 Inhibition of human alpha-thrombin 18053726

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
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor XI 1
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
18053726 10.1016/j.bmc.2007.11.015 Coagulation factor X 1

Data from ChEMBL 36 via Core Engine