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Assay Detail

CHEMBL5167633

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

Binding
Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Zhang J, Jiang H, Lin S, Wu D, Tian H, Jiang L, Cui Y, Jin J, Chen X, Xu H.
J Med Chem (2022) 65 : 8011 -8028
PubMed 35609190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.43 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3643413 LENIOLISIB 4.0 1 8.82
CHEMBL5192588 1 8.66
CHEMBL5203775 1 8.48
CHEMBL5178373 1 8.33
CHEMBL5204818 1 8.24
CHEMBL5178942 1 8.07
CHEMBL5174889 1 8.00
CHEMBL5188347 1 8.00
CHEMBL5177854 1 7.96
CHEMBL5175244 1 7.92
CHEMBL5179250 1 7.68
CHEMBL5205011 1 7.58
CHEMBL5196839 1 7.52
CHEMBL5199087 1 7.43
CHEMBL5179550 1 7.42
CHEMBL5190613 1 7.35
CHEMBL5185603 1 7.28
CHEMBL5182641 1 7.27
CHEMBL5171306 1 7.26
CHEMBL5194806 1 7.22
CHEMBL5205397 1 7.01
CHEMBL5208623 1 6.99
CHEMBL5202530 1 6.89
CHEMBL5188346 1 6.87
CHEMBL5208539 1 6.81
CHEMBL5184666 1 6.74
CHEMBL5181233 1 6.57
CHEMBL5202548 1 6.34
CHEMBL5206003 1 6.33
CHEMBL5187872 1 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3643413 LENIOLISIB IC50 = 1.5 nM 8.82
CHEMBL5192588 IC50 = 2.2 nM 8.66
CHEMBL5203775 IC50 = 3.3 nM 8.48
CHEMBL5178373 IC50 = 4.7 nM 8.33
CHEMBL5204818 IC50 = 5.7 nM 8.24
CHEMBL5178942 IC50 = 8.5 nM 8.07
CHEMBL5174889 IC50 = 10.0 nM 8.00
CHEMBL5188347 IC50 = 10.0 nM 8.00
CHEMBL5177854 IC50 = 11.0 nM 7.96
CHEMBL5175244 IC50 = 12.0 nM 7.92
CHEMBL5179250 IC50 = 21.0 nM 7.68
CHEMBL5205011 IC50 = 26.0 nM 7.58
CHEMBL5196839 IC50 = 30.0 nM 7.52
CHEMBL5199087 IC50 = 37.0 nM 7.43
CHEMBL5179550 IC50 = 38.0 nM 7.42
CHEMBL5190613 IC50 = 45.0 nM 7.35
CHEMBL5185603 IC50 = 53.0 nM 7.28
CHEMBL5182641 IC50 = 54.0 nM 7.27
CHEMBL5171306 IC50 = 55.0 nM 7.26
CHEMBL5194806 IC50 = 60.0 nM 7.22
CHEMBL5205397 IC50 = 97.5 nM 7.01
CHEMBL5208623 IC50 = 103.0 nM 6.99
CHEMBL5202530 IC50 = 128.0 nM 6.89
CHEMBL5188346 IC50 = 136.0 nM 6.87
CHEMBL5208539 IC50 = 156.0 nM 6.81
CHEMBL5184666 IC50 = 182.0 nM 6.74
CHEMBL5181233 IC50 = 269.0 nM 6.57
CHEMBL5202548 IC50 = 458.0 nM 6.34
CHEMBL5206003 IC50 = 465.0 nM 6.33
CHEMBL5187872 IC50 = 1014.0 nM 5.99