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Compound Detail

CHEMBL515107

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O=C(Nc1ccc(-n2ccccc2=O)cc1F)[C@H]1C[C@](O)(c2ccccc2)CN1C(=O)Nc1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL515107
Phase Preclinical
Structure Type MOL
InChI Key ZFOBYPBSJINJKI-VAVYLYDRSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

547.0
MW (Da)
4.76
ALogP
5
HBA
3
HBD
103.7
PSA (Ų)
0.34
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 C29H24ClFN4O4
MW 546.99
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.40

Activity Summary

IC50 1 meas. best 10.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
IC50 10.1 10.1 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X IC50 = 0.08 nM 10.1 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