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Compound Detail

CHEMBL4436648

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CS(=O)(=O)Nc1ccc(-c2cncc(/C=C3\SC(=N)NC3=O)c2)cc1

Basic Information

ChEMBL ID CHEMBL4436648
Phase Preclinical
Structure Type MOL
InChI Key AGHDPPGOJJYURV-AUWJEWJLSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
2.26
ALogP
6
HBA
3
HBD
112.0
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14N4O3S2
MW 374.45
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 6.57
Kd 1 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma
CHEMBL1770034
Kd 8.8 8.8 1.6 1
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
CHEMBL1795194
IC50 6.57 6.57 270.0 1
Phosphatidylinositol 5-phosphate 4-kinase type-2 beta
CHEMBL5667
IC50 5.77 5.77 1700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32298120 10.1021/acs.jmedchem.0c00227 Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha 4
32298120 10.1021/acs.jmedchem.0c00227 Phosphatidylinositol 5-phosphate 4-kinase type-2 beta 3
32298120 10.1021/acs.jmedchem.0c00227 No relevant target 2
32298120 10.1021/acs.jmedchem.0c00227 TGF-beta receptor type-2 2
32298120 10.1021/acs.jmedchem.0c00227 ADMET 1
32298120 10.1021/acs.jmedchem.0c00227 Activin receptor type-2A 1
32298120 10.1021/acs.jmedchem.0c00227 Activin receptor type-2B 1
32298120 10.1021/acs.jmedchem.0c00227 Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma 1

Data from ChEMBL 36 via Core Engine