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Assay Detail

CHEMBL1108787

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

Binding
Inhibition of mTOR
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Yu K, Zask A.
Bioorg Med Chem Lett (2010) 20 : 2648 -2653
PubMed 20223663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 9.13 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1091714 1 10.00
CHEMBL1091358 1 9.85
CHEMBL1091596 1 9.74
CHEMBL1092389 1 9.60
CHEMBL1092398 1 9.59
CHEMBL1091357 1 9.47
CHEMBL1091360 1 9.40
CHEMBL1091713 1 9.38
CHEMBL1091356 1 9.34
CHEMBL1091350 1 9.28
CHEMBL1091351 1 9.27
CHEMBL1091354 1 9.25
CHEMBL1091352 1 9.25
CHEMBL1092391 1 9.24
CHEMBL1092390 1 9.24
CHEMBL1091349 1 9.15
CHEMBL1091359 1 9.15
CHEMBL1091344 1 9.15
CHEMBL1092397 1 9.10
CHEMBL1091355 1 9.09
CHEMBL1091353 1 9.06
CHEMBL1092396 1 9.05
CHEMBL1092394 1 9.05
CHEMBL1091712 1 9.05
CHEMBL1088973 1 9.00
CHEMBL1092392 1 9.00
CHEMBL1092393 1 8.96
CHEMBL1091348 1 8.92
CHEMBL1076864 1 8.92
CHEMBL1091711 1 8.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1091714 IC50 = 0.1 nM 10.00
CHEMBL1091358 IC50 = 0.14 nM 9.85
CHEMBL1091596 IC50 = 0.18 nM 9.74
CHEMBL1092389 IC50 = 0.25 nM 9.60
CHEMBL1092398 IC50 = 0.26 nM 9.59
CHEMBL1091357 IC50 = 0.34 nM 9.47
CHEMBL1091360 IC50 = 0.4 nM 9.40
CHEMBL1091713 IC50 = 0.42 nM 9.38
CHEMBL1091356 IC50 = 0.46 nM 9.34
CHEMBL1091350 IC50 = 0.52 nM 9.28
CHEMBL1091351 IC50 = 0.535 nM 9.27
CHEMBL1091354 IC50 = 0.56 nM 9.25
CHEMBL1091352 IC50 = 0.56 nM 9.25
CHEMBL1092391 IC50 = 0.57 nM 9.24
CHEMBL1092390 IC50 = 0.57 nM 9.24
CHEMBL1091359 IC50 = 0.7 nM 9.15
CHEMBL1091349 IC50 = 0.7 nM 9.15
CHEMBL1091344 IC50 = 0.7 nM 9.15
CHEMBL1092397 IC50 = 0.8 nM 9.10
CHEMBL1091355 IC50 = 0.81 nM 9.09
CHEMBL1091353 IC50 = 0.88 nM 9.06
CHEMBL1092396 IC50 = 0.9 nM 9.05
CHEMBL1092394 IC50 = 0.89 nM 9.05
CHEMBL1091712 IC50 = 0.9 nM 9.05
CHEMBL1092392 IC50 = 1.0 nM 9.00
CHEMBL1088973 IC50 = 1.0 nM 9.00
CHEMBL1092393 IC50 = 1.1 nM 8.96
CHEMBL1091348 IC50 = 1.2 nM 8.92
CHEMBL1076864 IC50 = 1.2 nM 8.92
CHEMBL1091711 IC50 = 1.25 nM 8.90
CHEMBL1092395 IC50 = 1.6 nM 8.80
CHEMBL1091715 IC50 = 1.7 nM 8.77
CHEMBL1091345 IC50 = 5.4 nM 8.27
CHEMBL1091346 IC50 = 6.6 nM 8.18
CHEMBL1091347 IC50 = 8.8 nM 8.06