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Assay Detail

CHEMBL4410951

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

Binding
Inhibition of mTORC2 in human A431 cells assessed as AKT phosphorylation at S473 residue incubated for 3 hrs by HTRF assay
19
Total Activities
19
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

mTORC2 (CHEMBL4523999)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.
Ouvry G, Clary L, Tomas L, Aurelly M, Bonnary L, Borde E, Bouix-Peter C, Chantalat L, Defoin-Platel C, Deret S, Forissier M, Harris CS, Isabet T, Lamy L, Luzy AP, Pascau J, Soulet C, Taddei A, Taquet N, Thoreau E, Varvier E, Vial E, Hennequin LF.
ACS Med Chem Lett (2019) 10 : 1561 -1567
PubMed 31749911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.21 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564479 1 8.30
CHEMBL3545097 SAPANISERTIB 2.0 1 8.30
CHEMBL4529672 1 7.96
CHEMBL4549761 1 7.70
CHEMBL4572049 1 7.70
CHEMBL4588610 1 7.22
CHEMBL4538004 1 7.10
CHEMBL4538629 1 7.05
CHEMBL4517253 1 7.05
CHEMBL4585005 1 6.89
CHEMBL4461815 1 6.85
CHEMBL4441763 1 6.70
CHEMBL4475845 1 6.70
CHEMBL4456417 1 6.44
CHEMBL4525459 1 6.17
CHEMBL4440554 1 -
CHEMBL4475002 1 -
CHEMBL4451788 1 -
CHEMBL4522109 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564479 IC50 = 5.0 nM 8.30
CHEMBL3545097 SAPANISERTIB IC50 = 5.0 nM 8.30
CHEMBL4529672 IC50 = 11.0 nM 7.96
CHEMBL4549761 IC50 = 20.0 nM 7.70
CHEMBL4572049 IC50 = 20.0 nM 7.70
CHEMBL4588610 IC50 = 60.0 nM 7.22
CHEMBL4538004 IC50 = 80.0 nM 7.10
CHEMBL4538629 IC50 = 90.0 nM 7.05
CHEMBL4517253 IC50 = 90.0 nM 7.05
CHEMBL4585005 IC50 = 130.0 nM 6.89
CHEMBL4461815 IC50 = 140.0 nM 6.85
CHEMBL4441763 IC50 = 200.0 nM 6.70
CHEMBL4475845 IC50 = 200.0 nM 6.70
CHEMBL4456417 IC50 = 360.0 nM 6.44
CHEMBL4525459 IC50 = 680.0 nM 6.17
CHEMBL4440554 IC50 - -
CHEMBL4475002 IC50 - -
CHEMBL4451788 IC50 - -
CHEMBL4522109 IC50 - -