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Assay Detail

CHEMBL5519925

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

Binding
Binding affinity to mTORC1 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

mTORC1 (CHEMBL4296661)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Hu J, Fu S, Zhan Z, Zhang J.
Eur J Med Chem (2024) 265 : 116109 -116109
PubMed 38183777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.19 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1236962 OMIPALISIB 2.0 1 9.74
CHEMBL1091978 1 7.68
CHEMBL3813842 PAXALISIB 2.0 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1236962 OMIPALISIB Ki = 0.18 nM 9.74
CHEMBL1091978 Ki = 21.0 nM 7.68
CHEMBL3813842 PAXALISIB Ki = 70.0 nM 7.16