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Assay Detail

CHEMBL4199835

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Functional
Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MCF7
Confidence 1 — Organism
Curated By Intermediate

Target

MCF7 (CHEMBL387)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Shen S, He X, Yang Z, Zhang L, Liu Y, Zhang Z, Wang W, Liu W, Li Y, Huang D, Sun K, Ni X, Yang X, Chu X, Cui Y, Lv Q, Lan J, Zhou F.
ACS Med Chem Lett (2018) 9 : 719 -724
PubMed 30034607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.66 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211915 1 7.96
CHEMBL4211402 1 7.82
CHEMBL4208505 1 7.57
CHEMBL4218707 1 7.11
CHEMBL4207037 1 6.98
CHEMBL4206442 1 6.95
CHEMBL4214713 1 6.87
CHEMBL4213772 1 6.80
CHEMBL4203634 1 6.74
CHEMBL2017974 BUPARLISIB 3.0 1 6.69
CHEMBL4218171 1 6.67
CHEMBL4203109 1 6.65
CHEMBL4215969 1 6.55
CHEMBL4204166 1 6.54
CHEMBL4215235 1 6.53
CHEMBL4206215 1 6.47
CHEMBL4205959 1 6.39
CHEMBL4210822 1 6.36
CHEMBL4210301 1 6.29
CHEMBL4207389 1 6.29
CHEMBL4215841 1 6.24
CHEMBL4205938 1 6.22
CHEMBL4202499 1 6.05
CHEMBL4213112 1 5.94
CHEMBL4210320 1 5.82
CHEMBL4216218 1 -
CHEMBL4211255 1 -
CHEMBL4210843 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211915 IC50 = 11.0 nM 7.96
CHEMBL4211402 IC50 = 15.0 nM 7.82
CHEMBL4208505 IC50 = 27.0 nM 7.57
CHEMBL4218707 IC50 = 78.0 nM 7.11
CHEMBL4207037 IC50 = 104.0 nM 6.98
CHEMBL4206442 IC50 = 112.0 nM 6.95
CHEMBL4214713 IC50 = 134.0 nM 6.87
CHEMBL4213772 IC50 = 159.0 nM 6.80
CHEMBL4203634 IC50 = 184.0 nM 6.74
CHEMBL2017974 BUPARLISIB IC50 = 206.0 nM 6.69
CHEMBL4218171 IC50 = 214.0 nM 6.67
CHEMBL4203109 IC50 = 224.0 nM 6.65
CHEMBL4215969 IC50 = 283.0 nM 6.55
CHEMBL4204166 IC50 = 286.0 nM 6.54
CHEMBL4215235 IC50 = 295.0 nM 6.53
CHEMBL4206215 IC50 = 340.0 nM 6.47
CHEMBL4205959 IC50 = 408.0 nM 6.39
CHEMBL4210822 IC50 = 437.0 nM 6.36
CHEMBL4210301 IC50 = 512.0 nM 6.29
CHEMBL4207389 IC50 = 513.0 nM 6.29
CHEMBL4215841 IC50 = 571.5 nM 6.24
CHEMBL4205938 IC50 = 599.0 nM 6.22
CHEMBL4202499 IC50 = 897.0 nM 6.05
CHEMBL4213112 IC50 = 1139.0 nM 5.94
CHEMBL4210320 IC50 = 1513.0 nM 5.82
CHEMBL4216218 IC50 - -
CHEMBL4211255 IC50 - -
CHEMBL4210843 IC50 - -