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Compound Detail

CHEMBL269969

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CC(C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)N[C@H](C)c1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL269969
Phase Preclinical
Structure Type MOL
InChI Key RXLLECDUMUZHQF-CHQQOIJLSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

719.8
MW (Da)
4.38
ALogP
7
HBA
7
HBD
191.2
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 C32H47BrN8O4S
MW 719.75
Aromatic Rings 2
Heavy Atoms 46
NP-Likeness -0.44

Activity Summary

IC50 3 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 8.0 8.0 10.0 1
Prothrombin
CHEMBL204
IC50 6.01 6.01 980.0 1
Coagulation factor X
CHEMBL244
IC50 5.57 5.57 2700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 10.0 nM 8.0 Inhibition of human factor 11a 18053726
Prothrombin IC50 = 980.0 nM 6.01 Inhibition of human alpha-thrombin 18053726
Coagulation factor X IC50 = 2700.0 nM 5.57 Inhibition of human factor 10a 18053726

Literature References

PubMed DOI Target Context # Activities
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