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Compound Detail

CHEMBL395823

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Nc1noc2ccc(-n3nc(C(F)(F)F)cc3C(=O)NC3CCN(c4ccccc4CN4CCC[C@H]4O)CC3)cc12

Basic Information

ChEMBL ID CHEMBL395823
Phase Preclinical
Structure Type MOL
InChI Key IYCGPDFYFRTXIV-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

569.6
MW (Da)
3.93
ALogP
9
HBA
3
HBD
125.7
PSA (Ų)
0.32
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30F3N7O3
MW 569.59
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.36

Activity Summary

Ki 1 meas. best 9.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.14 9.14 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.04 ml/min.mg Homo sapiens
CL 36.67 mL.min-1.kg-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.73 nM 9.14 Inhibition of human factor 10a 17174550

Literature References

PubMed DOI Target Context # Activities
17174550 10.1016/j.bmcl.2006.11.071 Canis familiaris 2
17174550 10.1016/j.bmcl.2006.11.071 Coagulation factor X 1
17174550 10.1016/j.bmcl.2006.11.071 Plasma 1
17174550 10.1016/j.bmcl.2006.11.071 Caco-2 1
17174550 10.1016/j.bmcl.2006.11.071 Liver microsomes 1

Data from ChEMBL 36 via Core Engine