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Compound Detail

CHEMBL448927

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O=C(Nc1ccc(-n2ccccc2=O)cn1)[C@H]1C[C@](O)(c2ccccc2C(F)(F)F)CN1C(=O)Nc1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL448927
Phase Preclinical
Structure Type MOL
InChI Key DAHKACFDKZAKMT-QDPGVEIFSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

598.0
MW (Da)
5.04
ALogP
6
HBA
3
HBD
116.6
PSA (Ų)
0.30
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H23ClF3N5O4
MW 597.98
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.32

Activity Summary

IC50 1 meas. best 9.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 9.47 9.47 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.89 mL.min-1.kg-1 Rattus norvegicus
T1/2 1.9 hr Rattus norvegicus
T1/2 1.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.34 nM 9.47 Inhibition of human Factor-10a 19231206

Literature References

PubMed DOI Target Context # Activities
19231206 10.1016/j.bmc.2009.01.063 Rattus norvegicus 3
19231206 10.1016/j.bmc.2009.01.063 Coagulation factor X 1
19231206 10.1016/j.bmc.2009.01.063 Canis familiaris 1

Data from ChEMBL 36 via Core Engine