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Compound Detail

CHEMBL5280284

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N#CCn1c2ccc(O)cc2c2c3c(n4cccc4c21)C(=O)NC3=O

Basic Information

ChEMBL ID CHEMBL5280284
Phase Preclinical
Structure Type MOL
InChI Key PHEXTCXTBBPBOL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

330.3
MW (Da)
2.16
ALogP
6
HBA
2
HBD
99.5
PSA (Ų)
0.52
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H10N4O3
MW 330.30
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.42

Activity Summary

IC50 2 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 6.58 6.58 260.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 6.38 6.38 420.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33528252 10.1021/acs.jmedchem.0c01887 Dual specificity protein kinase CLK1 1
33528252 10.1021/acs.jmedchem.0c01887 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
33528252 10.1021/acs.jmedchem.0c01887 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine