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Compound Detail

CHEMBL3417246

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CC[C@]1(CO)O[C@@H](n2ccc(N)nc2=O)[C@H](F)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL3417246
Phase Preclinical
Structure Type MOL
InChI Key WRHBWEWELIFEKF-PKIKSRDPSA-N
3
Targets
3
Activities
2
Assay Types
9
PK Parameters
13
Publications
0
Known Names

Molecular Properties

273.3
MW (Da)
-0.81
ALogP
7
HBA
3
HBD
110.6
PSA (Ų)
0.66
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H16FN3O4
MW 273.26
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness 1.21

Activity Summary

EC50 2 meas. best 6.38
IC50 1 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Respiratory syncytial virus
CHEMBL612679
EC50 6.38 6.38 420.0 1
Unchecked
CHEMBL612545
IC50 6.22 6.22 600.0 1
NON-PROTEIN TARGET
CHEMBL3879801
EC50 5.1 5.1 8000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 4360.0 ng.hr.mL-1 Macaca fascicularis
AUC 3145.0 ng.hr.mL-1 Rattus norvegicus
AUC 2459.0 ng.hr.mL-1 Mesocricetus auratus
CL 19.2 mL.min-1.kg-1 Macaca fascicularis
CL 25.5 mL.min-1.kg-1 Rattus norvegicus
CL 34.1 mL.min-1.kg-1 Mesocricetus auratus
T1/2 7.52 hr Macaca fascicularis
T1/2 1.34 hr Rattus norvegicus
T1/2 1.23 hr Mesocricetus auratus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25667954 10.1021/jm5017279 ADMET 7
25667954 10.1021/jm5017279 Cynomolgus monkey 5
25667954 10.1021/jm5017279 Rattus norvegicus 5
25667954 10.1021/jm5017279 Syrian golden hamster 5
25667954 10.1021/jm5017279 Lung 2
25667954 10.1021/jm5017279 Respiratory syncytial virus 1
25667954 10.1021/jm5017279 HeLa 1
25667954 10.1021/jm5017279 A549 1
25978965 10.1016/j.bmcl.2015.04.073 NON-PROTEIN TARGET 1
25978965 10.1016/j.bmcl.2015.04.073 Unchecked 1
25978965 10.1016/j.bmcl.2015.04.073 DNA-directed RNA polymerase, mitochondrial 1
25978965 10.1016/j.bmcl.2015.04.073 DNA polymerase subunit gamma-1/gamma-2 1
25978965 10.1016/j.bmcl.2015.04.073 MT4 1

Data from ChEMBL 36 via Core Engine