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Assay Detail

CHEMBL3706089

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

Binding
mTOR Kinase Activity Assay: The mTOR kinase TR-FRET assay utilizes a physiologically relevant protein substrate for mTOR (4E-BP1, labeled with an acceptor fluorophore (Green Fluorescent Protein) and paired with a corresponding Tb-labeled phospho-specific antibody. The assay itself can be divided into two phases: the reaction phase and the detection phase.
ChEMBL ↗
596
Total Activities
574
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

5-alkynyl-pyrimidines
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 596 8.28 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3645910 — — 1 10.15
CHEMBL3645914 — — 1 9.70
CHEMBL3645963 — — 1 9.68
CHEMBL3645913 — — 1 9.60
CHEMBL3645911 — — 1 9.59
CHEMBL3643265 — — 1 9.57
CHEMBL3645967 — — 1 9.55
CHEMBL3645912 — — 1 9.54
CHEMBL3645974 — — 1 9.49
CHEMBL3643219 — — 1 9.46
CHEMBL3643272 — — 1 9.44
CHEMBL3645978 — — 1 9.41
CHEMBL3643222 — — 1 9.40
CHEMBL3645973 — — 1 9.35
CHEMBL3648886 — — 1 9.35
CHEMBL3643263 — — 1 9.34
CHEMBL3645926 — — 1 9.34
CHEMBL3645916 — — 1 9.33
CHEMBL3645966 — — 1 9.31
CHEMBL3645829 — — 1 9.29
CHEMBL3645832 — — 1 9.28
CHEMBL3645977 — — 1 9.28
CHEMBL3645821 — — 1 9.27
CHEMBL3645964 — — 1 9.25
CHEMBL3645975 — — 1 9.25
CHEMBL3645923 — — 1 9.24
CHEMBL3645965 — — 1 9.24
CHEMBL3645830 — — 1 9.23
CHEMBL3645877 — — 1 9.23
CHEMBL3641010 — — 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3645910 — IC50 = 0.07 nM 10.15
CHEMBL3645914 — IC50 = 0.2 nM 9.70
CHEMBL3645963 — IC50 = 0.21 nM 9.68
CHEMBL3645913 — IC50 = 0.25 nM 9.60
CHEMBL3645911 — IC50 = 0.26 nM 9.59
CHEMBL3643265 — IC50 = 0.27 nM 9.57
CHEMBL3645967 — IC50 = 0.28 nM 9.55
CHEMBL3645912 — IC50 = 0.29 nM 9.54
CHEMBL3645974 — IC50 = 0.32 nM 9.49
CHEMBL3643219 — IC50 = 0.35 nM 9.46
CHEMBL3643272 — IC50 = 0.36 nM 9.44
CHEMBL3645978 — IC50 = 0.39 nM 9.41
CHEMBL3643222 — IC50 = 0.4 nM 9.40
CHEMBL3645973 — IC50 = 0.45 nM 9.35
CHEMBL3648886 — IC50 = 0.45 nM 9.35
CHEMBL3645926 — IC50 = 0.46 nM 9.34
CHEMBL3643263 — IC50 = 0.46 nM 9.34
CHEMBL3645916 — IC50 = 0.47 nM 9.33
CHEMBL3645966 — IC50 = 0.49 nM 9.31
CHEMBL3645829 — IC50 = 0.51 nM 9.29
CHEMBL3645977 — IC50 = 0.52 nM 9.28
CHEMBL3645832 — IC50 = 0.53 nM 9.28
CHEMBL3645821 — IC50 = 0.54 nM 9.27
CHEMBL3645975 — IC50 = 0.56 nM 9.25
CHEMBL3645964 — IC50 = 0.56 nM 9.25
CHEMBL3645923 — IC50 = 0.57 nM 9.24
CHEMBL3645965 — IC50 = 0.58 nM 9.24
CHEMBL3645877 — IC50 = 0.59 nM 9.23
CHEMBL3645830 — IC50 = 0.59 nM 9.23
CHEMBL3641010 — IC50 = 0.6 nM 9.22
CHEMBL3645908 — IC50 = 0.64 nM 9.19
CHEMBL3648882 — IC50 = 0.66 nM 9.18
CHEMBL3645927 — IC50 = 0.67 nM 9.17
CHEMBL3645906 — IC50 = 0.67 nM 9.17
CHEMBL3645858 — IC50 = 0.68 nM 9.17
CHEMBL3645971 — IC50 = 0.68 nM 9.17
CHEMBL3645960 — IC50 = 0.68 nM 9.17
CHEMBL3645827 — IC50 = 0.7 nM 9.15
CHEMBL3645828 — IC50 = 0.71 nM 9.15
CHEMBL3645915 — IC50 = 0.73 nM 9.14
CHEMBL3645820 — IC50 = 0.73 nM 9.14
CHEMBL3641006 — IC50 = 0.74 nM 9.13
CHEMBL3645976 — IC50 = 0.76 nM 9.12
CHEMBL3645918 — IC50 = 0.8 nM 9.10
CHEMBL3643264 — IC50 = 0.8 nM 9.10
CHEMBL3645931 — IC50 = 0.81 nM 9.09
CHEMBL3641018 — IC50 = 0.82 nM 9.09
CHEMBL3641016 — IC50 = 0.84 nM 9.08
CHEMBL3645866 — IC50 = 0.87 nM 9.06
CHEMBL3641005 — IC50 = 0.88 nM 9.06