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Assay Detail

CHEMBL4370792

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

Binding
Inhibition of PI3K in rat Rat-1 cells assessed as decrease in AKT 1/2 phosphorylation at ser473 residues after 1 hr by AlphaScreen assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor.
Hamajima T, Takahashi F, Kato K, Sugano Y, Yamaki S, Suzuki D, Moritomo A, Kubo S, Nakamura K, Yamagami K, Yokoo K, Fukahori H.
Bioorg Med Chem (2019) 27 : 1056 -1064
PubMed 30755348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.08 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3643409 1 7.33
CHEMBL3643349 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3643409 IC50 = 47.0 nM 7.33
CHEMBL3643349 IC50 = 153.0 nM 6.82