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Compound Detail

CHEMBL3946030

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C/C=C/c1cccc2cc([C@H](C)NC(=O)c3c(N)nn4cccnc34)n(-c3ccccc3)c(=O)c12

Basic Information

ChEMBL ID CHEMBL3946030
Phase Preclinical
Structure Type MOL
InChI Key ZXUNWLPETOFNAZ-KQEHZQRSSA-N
4
Targets
15
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

464.5
MW (Da)
4.14
ALogP
7
HBA
2
HBD
107.3
PSA (Ų)
0.41
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 C27H24N6O2
MW 464.53
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -0.96

Activity Summary

IC50 15 meas. best 6.48

Target Activity Profile

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 330.0 nM 6.48 Inhibition of human recombinant full length N-terminal His-tagged PI3Kgamma expr... 27660692
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform IC50 = 2000.0 nM 5.7 Inhibition Assays: Class I PI3-Ks can be either purchased (p110α/p85α, p110β/p85... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform IC50 = 2000.0 nM 5.7 Inhibition Assays: Class I PI3-Ks can be either purchased (p110α/p85α, p110β/p85... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 2000.0 nM 5.7 Inhibition Assays: Class I PI3-Ks can be either purchased (p110α/p85α, p110β/p85... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 2000.0 nM 5.7 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 3000.0 nM 5.52 Inhibition Assays: Class I PI3-Ks can be either purchased (p110α/p85α, p110β/p85... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 3000.0 nM 5.52 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 3000.0 nM 5.52 PI3-Kinase HTRF Assay: A PI3-Kinase HTRF® assay kit (cat No. 33-016) purchased f... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform IC50 = 4000.0 nM 5.4 PI3K-delta Selective Assay: A compound's ability in selectively inhibiting PI3K-... -
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform IC50 = 5000.0 nM 5.3 PI3K-gamma Selective Assay: A compound's ability in selectively inhibiting PI3K-... -

Literature References

PubMed DOI Target Context # Activities
27660692 10.1021/acsmedchemlett.6b00238 PI3-kinase p110-delta/p85-alpha 1
27660692 10.1021/acsmedchemlett.6b00238 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1

Data from ChEMBL 36 via Core Engine