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Compound Detail

CHEMBL5286669

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O=C(Nc1cnccc1-c1ccccc1)c1ccnn2cc(-c3ccccc3)nc12

Basic Information

ChEMBL ID CHEMBL5286669
Phase Preclinical
Structure Type MOL
InChI Key UGFWJLOCVRHXSF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

391.4
MW (Da)
4.71
ALogP
5
HBA
1
HBD
72.2
PSA (Ų)
0.48
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17N5O
MW 391.43
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.46

Activity Summary

IC50 3 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 alpha
CHEMBL2850
IC50 8.96 8.96 1.1 1
Unchecked
CHEMBL612545
IC50 8.44 8.44 3.6 1
Microtubule-associated protein tau
CHEMBL1293224
IC50 6.04 6.04 910.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.003 - Mus musculus
Fu 0.001 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36950863 10.1021/acs.jmedchem.3c00133 ADMET 8
36950863 10.1021/acs.jmedchem.3c00133 Unchecked 1
36950863 10.1021/acs.jmedchem.3c00133 Glycogen synthase kinase-3 alpha 1
36950863 10.1021/acs.jmedchem.3c00133 Microtubule-associated protein tau 1

Data from ChEMBL 36 via Core Engine