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Compound Detail

CHEMBL395372

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COc1ccc(-n2nc(Cn3cnnn3)c3c2C(=O)N(c2ccc(-c4ccccc4CN4CC[C@@H](O)C4)cc2)CC3)cc1

Basic Information

ChEMBL ID CHEMBL395372
Phase Preclinical
Structure Type MOL
InChI Key XSEZTBVLOUTJTF-AREMUKBSSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
6
Publications
0
Known Names

Molecular Properties

576.7
MW (Da)
3.35
ALogP
10
HBA
1
HBD
114.4
PSA (Ų)
0.30
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H32N8O3
MW 576.66
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.29

Activity Summary

Ki 2 meas. best 9.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.07 9.07 0.8 1
Prothrombin
CHEMBL204
Ki 6.01 6.01 970.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 43.0 mL.min-1.kg-1 Canis lupus familiaris
F 7.0 % Canis lupus familiaris
T1/2 1.8 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.85 nM 9.07 Binding affinity to human F10a 17914785
Prothrombin Ki = 970.0 nM 6.01 Inhibition of human thrombin 17914785

Literature References

PubMed DOI Target Context # Activities
17914785 10.1021/jm070245n Canis familiaris 4
17914785 10.1021/jm070245n Prothrombin 1
17914785 10.1021/jm070245n Coagulation factor X 1
17914785 10.1021/jm070245n Plasma 1
17914785 10.1021/jm070245n Caco-2 1
17914785 10.1021/jm070245n Trypsin 1

Data from ChEMBL 36 via Core Engine