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Compound Detail

CHEMBL209599

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O=C(O)COc1cccc2c1CC[C@](O)(COC(=O)N(c1ccc(F)cc1)c1ccc(F)cc1)C2

Basic Information

ChEMBL ID CHEMBL209599
Phase Preclinical
Structure Type MOL
InChI Key JIJRVLZPUGGNNB-AREMUKBSSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

483.5
MW (Da)
4.62
ALogP
5
HBA
2
HBD
96.3
PSA (Ų)
0.51
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23F2NO6
MW 483.47
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.22

Activity Summary

IC50 1 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Homo sapiens
CHEMBL372
IC50 7.23 7.23 59.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1607.0 ng.hr.mL-1 Rattus norvegicus
CL 4.6 mL.min-1.kg-1 Rattus norvegicus
CL 30.3 mL.min-1.kg-1 Rattus norvegicus
Cmax 1189.32 nM Rattus norvegicus
F 29.5 % Rattus norvegicus
T1/2 3.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Homo sapiens IC50 = 59.0 nM 7.23 Inhibition of ADP-induced platelet aggregation in human platelet rich plasma 16824754

Literature References

PubMed DOI Target Context # Activities
16824754 10.1016/j.bmcl.2006.06.033 Rattus norvegicus 6
16824754 10.1016/j.bmcl.2006.06.033 Homo sapiens 1
16824754 10.1016/j.bmcl.2006.06.033 Liver microsomes 1

Data from ChEMBL 36 via Core Engine