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Assay Detail

CHEMBL4839370

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

Binding
Inhibition of PI3K in human MCF7 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 30 mins by fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Berger M, Wortmann L, Buchgraber P, Lücking U, Zitzmann-Kolbe S, Wengner AM, Bader B, Bömer U, Briem H, Eis K, Rehwinkel H, Bartels F, Moosmayer D, Eberspächer U, Lienau P, Hammer S, Schatz CA, Wang Q, Wang Q, Mumberg D, Nising CF, Siemeister G.
J Med Chem (2021) 64 : 12723 -12737
PubMed 34428039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.97 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860779 1 6.76
CHEMBL4875626 1 6.36
CHEMBL4871998 1 6.29
CHEMBL4850640 1 6.01
CHEMBL4851439 1 5.98
CHEMBL4860129 1 5.98
CHEMBL4849035 1 5.83
CHEMBL4873263 1 5.42
CHEMBL4867528 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860779 IC50 = 174.0 nM 6.76
CHEMBL4875626 IC50 = 439.0 nM 6.36
CHEMBL4871998 IC50 = 513.0 nM 6.29
CHEMBL4850640 IC50 = 985.0 nM 6.01
CHEMBL4851439 IC50 = 1050.0 nM 5.98
CHEMBL4860129 IC50 = 1050.0 nM 5.98
CHEMBL4849035 IC50 = 1490.0 nM 5.83
CHEMBL4873263 IC50 = 3780.0 nM 5.42
CHEMBL4867528 IC50 = 7530.0 nM 5.12