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Compound Detail

CHEMBL4796016

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O=C1NCc2ccc3c(-c4cccc(Cl)c4)c[nH]c3c21

Basic Information

ChEMBL ID CHEMBL4796016
Phase Preclinical
Structure Type MOL
InChI Key XZCWNSGWBUAUOO-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

282.7
MW (Da)
3.73
ALogP
1
HBA
2
HBD
44.9
PSA (Ų)
0.70
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11ClN2O
MW 282.73
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.20

Activity Summary

IC50 3 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK3
CHEMBL4226
IC50 7.55 7.55 28.0 1
Dual specificity protein kinase CLK1
CHEMBL4224
IC50 7.06 7.06 88.0 1
Dual specificity protein kinase CLK2
CHEMBL4225
IC50 6.29 6.29 510.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 U2OS 320
- 10.6019/CHEMBL5724801 HEK-293T 320
- 10.6019/CHEMBL5724801 Fibroblast 320
- 10.6019/CHEMBL5058564 U2OS 10
- 10.6019/CHEMBL5303304 HEK-293T 8
- 10.6019/CHEMBL5303304 U2OS 8
- 10.6019/CHEMBL5058564 HEK-293T 8
- 10.6019/CHEMBL5058564 Fibroblast 8
- 10.6019/CHEMBL5303304 Fibroblast 7
32787076 10.1021/acs.jmedchem.0c00898 Unchecked 2
- 10.6019/CHEMBL5060014 Bromodomain-containing protein 4 1
34519506 10.1021/acs.jmedchem.1c00985 Dual specificity protein kinase CLK3 1
- 10.6019/CHEMBL5060014 Transcription intermediary factor 1-alpha 1
- 10.6019/CHEMBL5060014 Fibroblast growth factor receptor 3 1
- 10.6019/CHEMBL5060014 Casein kinase I isoform delta 1
- 10.6019/CHEMBL5060014 Cyclin-dependent kinase 2 1
- 10.6019/CHEMBL5060014 Peregrin 1
32787076 10.1021/acs.jmedchem.0c00898 Dual specificity protein kinase CLK4 1
- 10.6019/CHEMBL5060014 Tyrosine-protein kinase ABL1 1
32787076 10.1021/acs.jmedchem.0c00898 Dual specificity protein kinase CLK3 1

Data from ChEMBL 36 via Core Engine