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Compound Detail

CHEMBL402980

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COc1cc(Cl)cc(C(=O)Nc2ccc(Cl)cn2)c1NC(=O)c1ccc(-n2ccccc2=O)cc1

Basic Information

ChEMBL ID CHEMBL402980
Phase Preclinical
Structure Type MOL
InChI Key KIUAYZXZFQAAHD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

509.4
MW (Da)
5.05
ALogP
6
HBA
2
HBD
102.3
PSA (Ų)
0.38
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H18Cl2N4O4
MW 509.35
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.58

Activity Summary

Ki 1 meas. best 10.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.89 10.89 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 11.17 mL.min-1.kg-1 Canis lupus familiaris
F 99.0 % Canis lupus familiaris
T1/2 0.7 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.013 nM 10.89 Inhibition of human factor 10a 18424044

Literature References

PubMed DOI Target Context # Activities
18424044 10.1016/j.bmcl.2008.03.092 Canis familiaris 4
18424044 10.1016/j.bmcl.2008.03.092 Coagulation factor X 1
18424044 10.1016/j.bmcl.2008.03.092 Plasma 1

Data from ChEMBL 36 via Core Engine