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Compound Detail

CHEMBL4795389

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COc1ccc(-c2c([C@H](C)Nc3nc(N)nc(N)c3C#N)c(-c3ccccc3)c(=O)n3cc(F)ccc23)cc1

Basic Information

ChEMBL ID CHEMBL4795389
Phase Preclinical
Structure Type MOL
InChI Key BQCMIJCXWCRQBL-INIZCTEOSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

521.6
MW (Da)
4.78
ALogP
9
HBA
3
HBD
144.3
PSA (Ų)
0.29
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H24FN7O2
MW 521.56
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -0.91

Activity Summary

IC50 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
IC50 7.77 7.77 17.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33297683 10.1021/acs.jmedchem.0c01264 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 4
33297683 10.1021/acs.jmedchem.0c01264 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 3
33297683 10.1021/acs.jmedchem.0c01264 ADMET 3
33297683 10.1021/acs.jmedchem.0c01264 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
33297683 10.1021/acs.jmedchem.0c01264 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1

Data from ChEMBL 36 via Core Engine