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Compound Detail

CHEMBL5282544

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O=[N+]([O-])c1ccccc1-n1cc(COc2cccc3cnc(Nc4cccc(Cl)c4)nc23)nn1

Basic Information

ChEMBL ID CHEMBL5282544
Phase Preclinical
Structure Type MOL
InChI Key XYFHSCKRPLMJIO-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

473.9
MW (Da)
5.09
ALogP
9
HBA
1
HBD
120.9
PSA (Ų)
0.26
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H16ClN7O3
MW 473.88
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.97

Activity Summary

IC50 5 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 7.96 7.96 11.0 1
Dual specificity protein kinase CLK4
CHEMBL4203
IC50 7.7 7.7 20.0 1
Dual specificity protein kinase CLK2
CHEMBL4225
IC50 7.57 7.57 27.0 1
MCF7
CHEMBL387
IC50 5.4 5.4 4000.0 1
PC-3
CHEMBL390
IC50 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34519506 10.1021/acs.jmedchem.1c00985 Dual specificity protein kinase CLK3 1
34519506 10.1021/acs.jmedchem.1c00985 Dual specificity protein kinase CLK1 1
34519506 10.1021/acs.jmedchem.1c00985 Dual specificity protein kinase CLK2 1
34519506 10.1021/acs.jmedchem.1c00985 Dual specificity protein kinase CLK4 1
34519506 10.1021/acs.jmedchem.1c00985 PC-3 1
34519506 10.1021/acs.jmedchem.1c00985 MCF7 1
34519506 10.1021/acs.jmedchem.1c00985 Unchecked 1

Data from ChEMBL 36 via Core Engine