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Assay Detail

CHEMBL4325293

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Binding
Inhibition of PI3Kdelta in human HL60 cell extract measured after 2 hrs by kinobeads based pull down assay
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a Key Selectivity Target.
Henley ZA, Amour A, Barton N, Bantscheff M, Bergamini G, Bertrand SM, Convery M, Down K, Dümpelfeld B, Edwards CD, Grandi P, Gore PM, Keeling S, Livia S, Mallett D, Maxwell A, Price M, Rau C, Reinhard FBM, Rowedder J, Rowland P, Taylor JA, Thomas DA, Hessel EM, Hamblin JN.
J Med Chem (2020) 63 : 638 -655
PubMed 31855425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.47 8.80
pIC50 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4518946 1 8.80
CHEMBL4449047 1 8.50
CHEMBL4447804 1 8.50
CHEMBL4436797 1 8.50
CHEMBL4466265 1 8.40
CHEMBL4561242 1 8.30
CHEMBL4579923 1 8.30
CHEMBL4521647 1 -
CHEMBL4545906 1 -
CHEMBL4553962 1 -
CHEMBL4533741 1 -
CHEMBL4580593 1 -
CHEMBL4436659 1 -
CHEMBL4448491 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4518946 IC50 = 1.585 nM 8.80
CHEMBL4449047 IC50 = 3.162 nM 8.50
CHEMBL4447804 IC50 = 3.162 nM 8.50
CHEMBL4436797 IC50 = 3.162 nM 8.50
CHEMBL4466265 IC50 = 3.981 nM 8.40
CHEMBL4561242 IC50 = 5.012 nM 8.30
CHEMBL4579923 IC50 = 5.012 nM 8.30
CHEMBL4521647 pIC50 - -
CHEMBL4545906 pIC50 - -
CHEMBL4553962 pIC50 - -
CHEMBL4533741 pIC50 - -
CHEMBL4580593 pIC50 - -
CHEMBL4436659 pIC50 - -
CHEMBL4448491 pIC50 - -