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Assay Detail

CHEMBL4325290

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Binding
Binding affinity to PI3Kdelta in human HL60 cell extract measured after 2 hrs by kinobeads based pull down assay
2
Total Activities
2
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

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
Kd 2 9.65 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4579923 1 9.70
CHEMBL4556087 1 9.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4579923 Kd = 0.1995 nM 9.70
CHEMBL4556087 Kd = 0.2512 nM 9.60