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Compound Detail

CHEMBL4438249

AMDIZALISIB
🧪 Phase II
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🧪 Phase II
C[C@H](Nc1ncnc(N)c1C#N)c1cc2ncc(Cl)n2nc1-c1ccccc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4438249
Name AMDIZALISIB
Phase Phase II
Structure Type MOL
InChI Key WKDBRCUUDXLTIM-NSHDSACASA-N

Known Names

Amdizalisib Hmpl-689
4
Targets
11
Activities
1
Assay Types
0
PK Parameters
3
Publications
2
Known Names
3
Indications

Molecular Properties

390.8
MW (Da)
3.47
ALogP
8
HBA
2
HBD
117.8
PSA (Ų)
0.55
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -lisib
USAN Year 2022

Extended Properties

Molecular Formula C19H15ClN8
MW 390.84
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.46

Indications

Lymphoma Lymphoma, Follicular Neoplasms

Activity Summary

IC50 11 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PI3-kinase p110-delta/p85-alpha
CHEMBL2111432
 IC50 9.52 9.52 0.3 1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
CHEMBL3130
 IC50 9.52 9.4467 0.3 3
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
CHEMBL3267
 IC50 7.42 7.3725 38.0 4
Phosphatidylinositol 3-kinase regulatory subunit beta
CHEMBL4437
 IC50 7.06 6.8967 87.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
PI3-kinase p110-delta/p85-alpha IC50 = 0.3 nM 9.52 Inhibition of N-terminal His6-tagged recombinant full length human p110delta/unt... 30582813
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 0.3 nM 9.52 Transcreener KINASE Assay: Briefly, the Transcreener KINASE Assay was designed a... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 0.3 nM 9.52 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 0.5 nM 9.3 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 38.0 nM 7.42 Inhibition of recombinant N-terminal His-tagged full length human PI3Kgamma expr... 30582813
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 38.0 nM 7.42 Transcreener KINASE Assay: Briefly, the Transcreener KINASE Assay was designed a... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 38.0 nM 7.42 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 59.0 nM 7.23 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -
Phosphatidylinositol 3-kinase regulatory subunit beta IC50 = 87.0 nM 7.06 Transcreener KINASE Assay: Briefly, the Transcreener KINASE Assay was designed a... -
Phosphatidylinositol 3-kinase regulatory subunit beta IC50 = 87.0 nM 7.06 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -
Phosphatidylinositol 3-kinase regulatory subunit beta IC50 = 272.0 nM 6.57 Fluorescent Determination of PI3K Enzyme Activity: PI3K kinases including p110α/... -

Literature References

PubMed DOI Target Context # Activities
30582813 10.1021/acs.jmedchem.8b01298 Unchecked 2
30582813 10.1021/acs.jmedchem.8b01298 PI3-kinase p110-delta/p85-alpha 1
30582813 10.1021/acs.jmedchem.8b01298 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1

Data from ChEMBL 36 via Core Engine