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Compound Detail

CHEMBL2376094

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COc1ncc(-c2cc3c(C)nc(N)nc3n([C@H]3CC[C@@H](OCO)CC3)c2=O)cc1F

Basic Information

ChEMBL ID CHEMBL2376094
Phase Preclinical
Structure Type MOL
InChI Key SAQMYGKYGQDHJG-OKILXGFUSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

429.4
MW (Da)
2.34
ALogP
9
HBA
2
HBD
125.4
PSA (Ų)
0.59
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24FN5O4
MW 429.45
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.47

Activity Summary

Ki 1 meas. best 8.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
CHEMBL2499
Ki 8.93 8.93 1.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 142.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23506825 10.1016/j.bmcl.2013.02.020 ADMET 1
23506825 10.1016/j.bmcl.2013.02.020 Liver microsomes 1
23506825 10.1016/j.bmcl.2013.02.020 RAC-alpha serine/threonine-protein kinase 1
23506825 10.1016/j.bmcl.2013.02.020 Serine/threonine-protein kinase mTOR 1
23506825 10.1016/j.bmcl.2013.02.020 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1

Data from ChEMBL 36 via Core Engine