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Assay Detail

CHEMBL4352646

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

Binding
Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.
Jia H, Dai G, Su W, Xiao K, Weng J, Zhang Z, Wang Q, Yuan T, Shi F, Zhang Z, Chen W, Sai Y, Wang J, Li X, Cai Y, Yu J, Ren P, Venable J, Rao T, Edwards JP, Bembenek SD.
J Med Chem (2019) 62 : 4936 -4948
PubMed 31033293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4548876 1 9.00
CHEMBL3039502 DUVELISIB 4.0 1 9.00
CHEMBL4549473 1 8.52
CHEMBL4522342 1 8.52
CHEMBL4574883 1 8.52
CHEMBL4530831 1 8.52
CHEMBL2216870 IDELALISIB 4.0 1 8.40
CHEMBL4463472 1 8.30
CHEMBL4467526 1 7.80
CHEMBL4445566 1 7.68
CHEMBL4468887 1 7.68
CHEMBL4471912 1 -
CHEMBL4446047 1 -
CHEMBL4520300 1 -
CHEMBL4443601 1 -
CHEMBL4446644 1 -
CHEMBL4514752 1 -
CHEMBL4442420 1 -
CHEMBL4438693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4548876 IC50 = 1.0 nM 9.00
CHEMBL3039502 DUVELISIB IC50 = 1.0 nM 9.00
CHEMBL4549473 IC50 = 3.0 nM 8.52
CHEMBL4522342 IC50 = 3.0 nM 8.52
CHEMBL4574883 IC50 = 3.0 nM 8.52
CHEMBL4530831 IC50 = 3.0 nM 8.52
CHEMBL2216870 IDELALISIB IC50 = 4.0 nM 8.40
CHEMBL4463472 IC50 = 5.0 nM 8.30
CHEMBL4467526 IC50 = 16.0 nM 7.80
CHEMBL4445566 IC50 = 21.0 nM 7.68
CHEMBL4468887 IC50 = 21.0 nM 7.68
CHEMBL4471912 IC50 - -
CHEMBL4446047 IC50 - -
CHEMBL4520300 IC50 - -
CHEMBL4443601 IC50 - -
CHEMBL4446644 IC50 - -
CHEMBL4514752 IC50 - -
CHEMBL4442420 IC50 - -
CHEMBL4438693 IC50 - -