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Compound Detail

CHEMBL237228

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CCN(CC)Cc1ccccc1-c1ccc(N2CCc3c(C(N)=O)nn(-c4ccc(OC)cc4)c3C2=O)cc1

Basic Information

ChEMBL ID CHEMBL237228
Phase Preclinical
Structure Type MOL
InChI Key VTHIZWRLBYQAKK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
5
Publications
0
Known Names

Molecular Properties

523.6
MW (Da)
4.69
ALogP
6
HBA
1
HBD
93.7
PSA (Ų)
0.34
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H33N5O3
MW 523.64
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.07

Activity Summary

Ki 1 meas. best 10.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 10.1 10.1 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 40.0 mL.min-1.kg-1 Canis lupus familiaris
F 20.0 % Canis lupus familiaris
T1/2 3.7 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.08 nM 10.1 Binding affinity to human F10a 17914785

Literature References

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

Data from ChEMBL 36 via Core Engine