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Assay Detail

CHEMBL3293000

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

Binding
Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological evaluation of imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyridines as new inhibitors of the Wnt/β-catenin signaling.
Cosimelli B, Laneri S, Ostacolo C, Sacchi A, Severi E, Porcù E, Rampazzo E, Moro E, Basso G, Viola G.
Eur J Med Chem (2014) 83 : 45 -56
PubMed 24950489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.55 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3288551 1 5.21
CHEMBL3288555 1 5.01
CHEMBL3288549 1 4.98
CHEMBL3288553 1 4.96
CHEMBL3288545 1 4.84
CHEMBL3288550 1 4.79
CHEMBL3288558 1 4.75
CHEMBL2312139 1 4.73
CHEMBL3288554 1 4.71
CHEMBL3288539 1 4.65
CHEMBL3288556 1 4.64
CHEMBL3288559 1 4.62
CHEMBL562310 1 4.61
CHEMBL3288540 1 4.51
CHEMBL3288547 1 4.46
CHEMBL3288543 1 4.45
CHEMBL3288557 1 4.38
CHEMBL3288541 1 4.37
CHEMBL3288538 1 4.33
CHEMBL3288552 1 4.28
CHEMBL3288542 1 4.26
CHEMBL3288544 1 4.24
CHEMBL3288548 1 4.17
CHEMBL3288535 1 4.14
CHEMBL3288546 1 4.14
CHEMBL257487 1 4.09
CHEMBL3288560 1 -
CHEMBL3288537 1 -
CHEMBL3288536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3288551 IC50 = 6200.0 nM 5.21
CHEMBL3288555 IC50 = 9700.0 nM 5.01
CHEMBL3288549 IC50 = 10400.0 nM 4.98
CHEMBL3288553 IC50 = 11100.0 nM 4.96
CHEMBL3288545 IC50 = 14300.0 nM 4.84
CHEMBL3288550 IC50 = 16100.0 nM 4.79
CHEMBL3288558 IC50 = 17800.0 nM 4.75
CHEMBL2312139 IC50 = 18700.0 nM 4.73
CHEMBL3288554 IC50 = 19500.0 nM 4.71
CHEMBL3288539 IC50 = 22300.0 nM 4.65
CHEMBL3288556 IC50 = 23100.0 nM 4.64
CHEMBL3288559 IC50 = 24100.0 nM 4.62
CHEMBL562310 IC50 = 24400.0 nM 4.61
CHEMBL3288540 IC50 = 30700.0 nM 4.51
CHEMBL3288547 IC50 = 34600.0 nM 4.46
CHEMBL3288543 IC50 = 35600.0 nM 4.45
CHEMBL3288557 IC50 = 42200.0 nM 4.38
CHEMBL3288541 IC50 = 43000.0 nM 4.37
CHEMBL3288538 IC50 = 46200.0 nM 4.33
CHEMBL3288552 IC50 = 52600.0 nM 4.28
CHEMBL3288542 IC50 = 54300.0 nM 4.26
CHEMBL3288544 IC50 = 57800.0 nM 4.24
CHEMBL3288548 IC50 = 67000.0 nM 4.17
CHEMBL3288535 IC50 = 72200.0 nM 4.14
CHEMBL3288546 IC50 = 72200.0 nM 4.14
CHEMBL257487 IC50 = 81800.0 nM 4.09
CHEMBL3288560 IC50 > 100000.0 nM -
CHEMBL3288537 IC50 > 100000.0 nM -
CHEMBL3288536 IC50 > 100000.0 nM -