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Compound Detail

CHEMBL1081904

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COc1ccc(Oc2ncnc(N3CCC(Oc4ncc(F)c(N)n4)CC3)c2F)c(C#N)c1

Basic Information

ChEMBL ID CHEMBL1081904
Phase Preclinical
Structure Type MOL
InChI Key BEESLPAFNGNTIJ-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

455.4
MW (Da)
2.85
ALogP
10
HBA
1
HBD
132.3
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19F2N7O3
MW 455.43
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.21

Activity Summary

EC50 1 meas. best 8.3
IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Deoxycytidine kinase
CHEMBL2447
IC50 8.7 8.7 2.0 1
Deoxycytidine kinase
CHEMBL2447
EC50 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 107481.48 ng.hr.mL-1 Mus musculus
CL 3.3 mL.min-1.kg-1 Mus musculus
F 100.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19836229 10.1016/j.bmcl.2009.09.082 Mus musculus 4
19836229 10.1016/j.bmcl.2009.09.082 Deoxycytidine kinase 2

Data from ChEMBL 36 via Core Engine