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Assay Detail

CHEMBL4845571

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

Binding
Inhibition of mTOR (unknown origin) by LanthaScreen assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL2842)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.
Martínez-González S, Alvarez RM, Martín JI, García AB, Riesco-Fagundo C, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Albarrán MI, Gómez-Casero E, Cebriá A, Aguirre E, Ajenjo N, Cebrián D, Di Geronimo B, Cunningham D, O'Neill M, Dave HPG, Blanco-Aparicio C, Pastor J.
ACS Med Chem Lett (2021) 12 : 1794 -1801
PubMed 34795869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.50 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1236962 OMIPALISIB 2.0 1 8.90
CHEMBL4878958 1 7.13
CHEMBL4851911 1 7.09
CHEMBL4860369 1 6.86
CHEMBL4868512 1 6.76
CHEMBL4876895 1 6.71
CHEMBL4874628 1 6.22
CHEMBL4869487 1 5.69
CHEMBL4854645 1 5.68
CHEMBL4866896 1 5.25
CHEMBL4862404 1 5.24
CHEMBL4869696 1 -
CHEMBL4851433 1 -
CHEMBL4871634 1 -
CHEMBL4859036 1 -
CHEMBL4857792 1 -
CHEMBL4870601 1 -
CHEMBL4854392 1 -
CHEMBL4857726 1 -
CHEMBL4868086 1 -
CHEMBL4854225 1 -
CHEMBL4866710 1 -
CHEMBL4860117 1 -
CHEMBL4876693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1236962 OMIPALISIB IC50 = 1.25 nM 8.90
CHEMBL4878958 IC50 = 74.53 nM 7.13
CHEMBL4851911 IC50 = 80.88 nM 7.09
CHEMBL4860369 IC50 = 138.17 nM 6.86
CHEMBL4868512 IC50 = 175.33 nM 6.76
CHEMBL4876895 IC50 = 197.33 nM 6.71
CHEMBL4874628 IC50 = 604.0 nM 6.22
CHEMBL4869487 IC50 = 2030.0 nM 5.69
CHEMBL4854645 IC50 = 2100.0 nM 5.68
CHEMBL4866896 IC50 = 5570.0 nM 5.25
CHEMBL4862404 IC50 = 5700.0 nM 5.24
CHEMBL4869696 IC50 > 10000.0 nM -
CHEMBL4851433 IC50 > 10000.0 nM -
CHEMBL4871634 IC50 > 10000.0 nM -
CHEMBL4859036 IC50 > 10000.0 nM -
CHEMBL4857792 IC50 > 10000.0 nM -
CHEMBL4870601 IC50 > 10000.0 nM -
CHEMBL4854392 IC50 > 10000.0 nM -
CHEMBL4857726 IC50 > 10000.0 nM -
CHEMBL4868086 IC50 > 10000.0 nM -
CHEMBL4854225 IC50 > 10000.0 nM -
CHEMBL4866710 IC50 > 10000.0 nM -
CHEMBL4860117 IC50 > 10000.0 nM -
CHEMBL4876693 IC50 > 1000.0 nM -