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Assay Detail

CHEMBL4428799

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of PI3K p110alpha/p85 (unknown origin) using PIP2/ATP as substrate after 1 hr by kinase glo luminescent assay
29
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, Synthesis, and Biological Evaluation of Substituted Pyrimidines as Potential Phosphatidylinositol 3-Kinase (PI3K) Inhibitors.
Zhang JQ, Luo YJ, Xiong YS, Yu Y, Tu ZC, Long ZJ, Lai XJ, Chen HX, Luo Y, Weng J, Lu G.
J Med Chem (2016) 59 : 7268 -7274
PubMed 27427973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.01 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573339 PI-103 1 8.13
CHEMBL4555071 1 7.75
CHEMBL4548366 1 7.64
CHEMBL4522487 1 7.58
CHEMBL2017974 BUPARLISIB 3.0 1 7.55
CHEMBL4446205 2 7.51
CHEMBL4442758 1 7.51
CHEMBL4460361 2 7.50
CHEMBL4453932 1 7.42
CHEMBL4455733 1 7.23
CHEMBL4540522 1 7.22
CHEMBL4575186 1 7.21
CHEMBL4457773 1 7.04
CHEMBL4528366 1 6.93
CHEMBL4457370 1 6.93
CHEMBL4447129 1 6.89
CHEMBL4555749 1 6.65
CHEMBL4463279 1 6.43
CHEMBL4593426 1 6.25
CHEMBL4444148 1 6.05
CHEMBL4462863 1 5.24
CHEMBL4560668 1 5.02
CHEMBL4517113 1 -
CHEMBL4483565 1 -
CHEMBL4438022 1 -
CHEMBL4445769 1 -
CHEMBL4450205 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573339 PI-103 IC50 = 7.4 nM 8.13
CHEMBL4555071 IC50 = 18.0 nM 7.75
CHEMBL4548366 IC50 = 23.0 nM 7.64
CHEMBL4522487 IC50 = 26.0 nM 7.58
CHEMBL2017974 BUPARLISIB IC50 = 28.0 nM 7.55
CHEMBL4442758 IC50 = 31.0 nM 7.51
CHEMBL4446205 IC50 = 31.0 nM 7.51
CHEMBL4460361 IC50 = 32.0 nM 7.50
CHEMBL4446205 IC50 = 35.0 nM 7.46
CHEMBL4453932 IC50 = 38.0 nM 7.42
CHEMBL4455733 IC50 = 59.0 nM 7.23
CHEMBL4540522 IC50 = 60.0 nM 7.22
CHEMBL4575186 IC50 = 61.0 nM 7.21
CHEMBL4460361 IC50 = 68.0 nM 7.17
CHEMBL4457773 IC50 = 91.0 nM 7.04
CHEMBL4528366 IC50 = 118.0 nM 6.93
CHEMBL4457370 IC50 = 117.0 nM 6.93
CHEMBL4447129 IC50 = 128.0 nM 6.89
CHEMBL4555749 IC50 = 224.0 nM 6.65
CHEMBL4463279 IC50 = 375.0 nM 6.43
CHEMBL4593426 IC50 = 568.0 nM 6.25
CHEMBL4444148 IC50 = 896.0 nM 6.05
CHEMBL4462863 IC50 = 5751.0 nM 5.24
CHEMBL4560668 IC50 = 9530.0 nM 5.02
CHEMBL4483565 IC50 > 10000.0 nM -
CHEMBL4438022 IC50 > 10000.0 nM -
CHEMBL4517113 IC50 > 10000.0 nM -
CHEMBL4445769 IC50 > 10000.0 nM -
CHEMBL4450205 IC50 > 10000.0 nM -