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Compound Detail

CHEMBL515156

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CC[C@@]1(O)C[C@H](C(=O)Nc2ccc(-n3cccc(C)c3=O)cc2F)N(C(=O)Nc2ccc(Cl)cc2)C1

Basic Information

ChEMBL ID CHEMBL515156
Phase Preclinical
Structure Type MOL
InChI Key LSOZSNOCDGEDMN-ATIYNZHBSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

513.0
MW (Da)
4.32
ALogP
5
HBA
3
HBD
103.7
PSA (Ų)
0.47
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26ClFN4O4
MW 512.97
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.50

Activity Summary

IC50 1 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 9.3 9.3 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 5.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.5 nM 9.3 Inhibition of human Factor-10a 19231206

Literature References

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

Data from ChEMBL 36 via Core Engine