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Compound Detail

CHEMBL5268185

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O=C(Nc1cnccc1-c1ccc(F)cc1C(F)(F)F)c1ccnc(NC(=O)C2CC2)c1

Basic Information

ChEMBL ID CHEMBL5268185
Phase Preclinical
Structure Type MOL
InChI Key COJODIOMIPYEGM-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

444.4
MW (Da)
4.90
ALogP
4
HBA
2
HBD
84.0
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16F4N4O2
MW 444.39
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.55

Activity Summary

IC50 3 meas. best 9.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 alpha
CHEMBL2850
IC50 9.77 9.77 0.2 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 9.06 8.455 0.9 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26751161 10.1021/acs.jmedchem.5b01550 ADMET 3
26751161 10.1021/acs.jmedchem.5b01550 Glycogen synthase kinase-3 beta 2
26751161 10.1021/acs.jmedchem.5b01550 ATP-dependent translocase ABCB1 1
26751161 10.1021/acs.jmedchem.5b01550 Glycogen synthase kinase-3 alpha 1

Data from ChEMBL 36 via Core Engine