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Assay Detail

CHEMBL4233147

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

Functional
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
14
Total Activities
14
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

Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.
Liu Y, Xia Q, Fang L.
Bioorg Med Chem (2018) 26 : 3992 -4000
PubMed 29945756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.17 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4238656 1 8.22
CHEMBL1801204 AZD-8055 1.0 1 7.57
CHEMBL4239712 1 7.51
CHEMBL4250280 1 7.27
CHEMBL4246481 1 7.14
CHEMBL4240170 1 7.11
CHEMBL4248529 1 6.73
CHEMBL4246121 1 6.65
CHEMBL4251185 1 6.35
CHEMBL4239569 1 -
CHEMBL4239931 1 -
CHEMBL4244147 1 -
CHEMBL4246923 1 -
CHEMBL4242668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4238656 IC50 = 6.0 nM 8.22
CHEMBL1801204 AZD-8055 IC50 = 27.0 nM 7.57
CHEMBL4239712 IC50 = 31.0 nM 7.51
CHEMBL4250280 IC50 = 54.0 nM 7.27
CHEMBL4246481 IC50 = 72.0 nM 7.14
CHEMBL4240170 IC50 = 77.3 nM 7.11
CHEMBL4248529 IC50 = 185.7 nM 6.73
CHEMBL4246121 IC50 = 225.0 nM 6.65
CHEMBL4251185 IC50 = 443.0 nM 6.35
CHEMBL4239569 IC50 > 1000.0 nM -
CHEMBL4239931 IC50 > 1000.0 nM -
CHEMBL4244147 IC50 > 1000.0 nM -
CHEMBL4246923 IC50 > 1000.0 nM -
CHEMBL4242668 IC50 > 1000.0 nM -