Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4831259

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

Binding
Inhibition of PI3K/Akt/mTOR pathway in human MDA-MB-468 cells assessed as reduction in S6 phosphorylation incubated for 15 to 20 mins by Alexa Fluor 488 staining based assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
DeSelm L, Huck B, Lan R, Neagu C, Potnick J, Xiao Y, Chen X, Jones R, Richardson TE, Heasley BH, Haxell T, Moore J, Tian H, Georgi K, Rohdich F, Sutton A, Johnson T, Mochalkin I, Jackson J, Lin J, Crowley L, Machl A, Clark A, Wilker E, Sherer B, Goutopoulos A.
J Med Chem (2021) 64 : 14603 -14619
PubMed 34596404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.54 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3675442 1 10.10
CHEMBL4878044 1 8.80
CHEMBL3680521 1 8.04
CHEMBL4871106 RUPITASERTIB 2.0 1 7.96
CHEMBL3675415 1 7.60
CHEMBL4855657 1 7.60
CHEMBL4871853 1 7.55
CHEMBL4846712 1 7.37
CHEMBL4856439 1 7.37
CHEMBL3685329 1 7.35
CHEMBL4876446 1 7.25
CHEMBL4854144 1 7.14
CHEMBL4860970 1 7.13
CHEMBL4851020 1 7.12
CHEMBL4875416 1 6.99
CHEMBL4869229 1 6.74
CHEMBL4846770 1 6.15
CHEMBL4857965 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3675442 IC50 = 0.08 nM 10.10
CHEMBL4878044 IC50 = 1.6 nM 8.80
CHEMBL3680521 IC50 = 9.17 nM 8.04
CHEMBL4871106 RUPITASERTIB IC50 = 11.0 nM 7.96
CHEMBL3675415 IC50 = 25.0 nM 7.60
CHEMBL4855657 IC50 = 25.0 nM 7.60
CHEMBL4871853 IC50 = 28.0 nM 7.55
CHEMBL4846712 IC50 = 43.0 nM 7.37
CHEMBL4856439 IC50 = 43.0 nM 7.37
CHEMBL3685329 IC50 = 45.0 nM 7.35
CHEMBL4876446 IC50 = 56.0 nM 7.25
CHEMBL4854144 IC50 = 72.0 nM 7.14
CHEMBL4860970 IC50 = 74.0 nM 7.13
CHEMBL4851020 IC50 = 76.0 nM 7.12
CHEMBL4875416 IC50 = 103.0 nM 6.99
CHEMBL4869229 IC50 = 183.0 nM 6.74
CHEMBL4846770 IC50 = 702.0 nM 6.15
CHEMBL4857965 IC50 > 1000.0 nM -