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Compound Detail

CHEMBL4171209

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O=C(NCCN1CCOCC1)Nc1cccc(-c2ccc3nc(NC(=O)C4CC4)sc3n2)c1

Basic Information

ChEMBL ID CHEMBL4171209
Phase Preclinical
Structure Type MOL
InChI Key NVIJYBFQLMPXOI-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

466.6
MW (Da)
3.16
ALogP
7
HBA
3
HBD
108.5
PSA (Ų)
0.49
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N6O3S
MW 466.57
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -2.49

Activity Summary

IC50 1 meas. best 5.46
Ki 1 meas. best 5.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
Ki 5.78 5.78 1680.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 5.46 5.46 3500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30095246 10.1021/acs.jmedchem.7b01847 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 5
30095246 10.1021/acs.jmedchem.7b01847 Platelet-derived growth factor receptor beta 1
30095246 10.1021/acs.jmedchem.7b01847 Dual specificity protein kinase CLK2 1
30095246 10.1021/acs.jmedchem.7b01847 Tyrosine-protein kinase ABL1 1
30095246 10.1021/acs.jmedchem.7b01847 Platelet-derived growth factor receptor alpha 1

Data from ChEMBL 36 via Core Engine