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Assay Detail

CHEMBL4000379

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Functional
Antiproliferative activity against human HCT116 cells harboring PI3CA H1047R mutant after 72 hrs by MTT assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.
Zhang H, Xin MH, Xie XX, Mao S, Zuo SJ, Lu SM, Zhang SQ.
Bioorg Med Chem (2015) 23 : 7765 -7776
PubMed 26652969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.79 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1879463 DACTOLISIB 3.0 1 6.25
CHEMBL4089891 1 6.22
CHEMBL4097092 1 6.18
CHEMBL4088969 1 6.17
CHEMBL4097625 1 6.15
CHEMBL4060710 1 6.02
CHEMBL4098014 1 5.99
CHEMBL4105333 1 5.94
CHEMBL4096535 1 5.92
CHEMBL4082582 1 5.91
CHEMBL4079071 1 5.90
CHEMBL4084993 1 5.90
CHEMBL4068201 1 5.89
CHEMBL4084553 1 5.89
CHEMBL4075213 1 5.87
CHEMBL4062875 1 5.87
CHEMBL4089383 1 5.85
CHEMBL4063347 1 5.84
CHEMBL4070327 1 5.84
CHEMBL4081081 1 5.82
CHEMBL4091254 1 5.74
CHEMBL4095616 1 5.70
CHEMBL4098987 1 5.58
CHEMBL4069304 1 5.57
CHEMBL4080959 1 5.56
CHEMBL4059556 1 5.55
CHEMBL4081506 1 5.53
CHEMBL4088838 1 5.39
CHEMBL4070452 1 5.33
CHEMBL4070920 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1879463 DACTOLISIB IC50 = 560.0 nM 6.25
CHEMBL4089891 IC50 = 600.0 nM 6.22
CHEMBL4097092 IC50 = 660.0 nM 6.18
CHEMBL4088969 IC50 = 670.0 nM 6.17
CHEMBL4097625 IC50 = 710.0 nM 6.15
CHEMBL4060710 IC50 = 960.0 nM 6.02
CHEMBL4098014 IC50 = 1030.0 nM 5.99
CHEMBL4105333 IC50 = 1150.0 nM 5.94
CHEMBL4096535 IC50 = 1200.0 nM 5.92
CHEMBL4082582 IC50 = 1220.0 nM 5.91
CHEMBL4079071 IC50 = 1250.0 nM 5.90
CHEMBL4084993 IC50 = 1250.0 nM 5.90
CHEMBL4068201 IC50 = 1290.0 nM 5.89
CHEMBL4084553 IC50 = 1300.0 nM 5.89
CHEMBL4062875 IC50 = 1350.0 nM 5.87
CHEMBL4075213 IC50 = 1350.0 nM 5.87
CHEMBL4089383 IC50 = 1420.0 nM 5.85
CHEMBL4063347 IC50 = 1460.0 nM 5.84
CHEMBL4070327 IC50 = 1450.0 nM 5.84
CHEMBL4081081 IC50 = 1530.0 nM 5.82
CHEMBL4091254 IC50 = 1820.0 nM 5.74
CHEMBL4095616 IC50 = 2020.0 nM 5.70
CHEMBL4098987 IC50 = 2640.0 nM 5.58
CHEMBL4069304 IC50 = 2690.0 nM 5.57
CHEMBL4080959 IC50 = 2750.0 nM 5.56
CHEMBL4059556 IC50 = 2800.0 nM 5.55
CHEMBL4081506 IC50 = 2950.0 nM 5.53
CHEMBL4088838 IC50 = 4060.0 nM 5.39
CHEMBL4070452 IC50 = 4720.0 nM 5.33
CHEMBL4070920 IC50 = 4740.0 nM 5.32
CHEMBL4067753 IC50 = 4880.0 nM 5.31
CHEMBL4061827 IC50 = 6090.0 nM 5.21