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Compound Detail

CHEMBL4450504

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Fc1ccc2[nH]ccc2c1-c1nc(N2CCOCC2)c2sc(CN3CCN(CC4CC4)CC3)cc2n1

Basic Information

ChEMBL ID CHEMBL4450504
Phase Preclinical
Structure Type MOL
InChI Key YDNOHCOYQVZOMC-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
4.34
ALogP
7
HBA
1
HBD
60.5
PSA (Ų)
0.42
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C27H31FN6OS
MW 506.65
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.54

Activity Summary

IC50 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
IC50 7.82 7.82 15.0 1
PI3K p110 beta/p85 alpha
CHEMBL3038510
IC50 5.97 5.97 1078.0 1
PI3-kinase p110-alpha/p85-alpha
CHEMBL2111367
IC50 5.64 5.64 2299.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30530193 10.1016/j.ejmech.2018.11.072 Unchecked 3
30530193 10.1016/j.ejmech.2018.11.072 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
30530193 10.1016/j.ejmech.2018.11.072 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
30530193 10.1016/j.ejmech.2018.11.072 PI3K p110 beta/p85 alpha 1
30530193 10.1016/j.ejmech.2018.11.072 PI3-kinase p110-alpha/p85-alpha 1

Data from ChEMBL 36 via Core Engine