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Compound Detail

CHEMBL174558

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CN(Cc1ccc(C(=O)Nc2ccc(Cl)cc2C(=O)Nc2ccc(Cl)cn2)cc1)C(=N)N

Basic Information

ChEMBL ID CHEMBL174558
Phase Preclinical
Structure Type MOL
InChI Key RTAQWGSGYVZCLM-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
4.22
ALogP
4
HBA
4
HBD
124.2
PSA (Ų)
0.32
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20Cl2N6O2
MW 471.35
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.60

Activity Summary

IC50 2 meas. best 9.0
Ki 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.0 10.0 0.1 1
Coagulation factor X
CHEMBL244
IC50 9.0 9.0 1.0 1
Plasma kallikrein
CHEMBL2000
IC50 6.42 6.42 380.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 1.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15013007 10.1016/j.bmcl.2003.11.080 Coagulation factor X 2
15013007 10.1016/j.bmcl.2003.11.080 Prothrombin 1
15013007 10.1016/j.bmcl.2003.11.080 Tissue-type plasminogen activator 1
15013007 10.1016/j.bmcl.2003.11.080 Serine protease 1 1
15013007 10.1016/j.bmcl.2003.11.080 Vitamin K-dependent protein C 1
15013007 10.1016/j.bmcl.2003.11.080 Plasminogen 1
15013007 10.1016/j.bmcl.2003.11.080 Homo sapiens 1
15013007 10.1016/j.bmcl.2003.11.080 Rattus norvegicus 1
15013007 10.1016/j.bmcl.2003.11.080 Plasma kallikrein 1

Data from ChEMBL 36 via Core Engine