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Assay Detail

CHEMBL1047013

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

Functional
Growth inhibition of human Tcf22C11 cells transiently transfected with pGL3-Tcf4-luc and SV40-R-luc after 24 hrs by luciferase reporter assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Tcf22C11
Confidence 1 — Organism
Curated By Autocuration

Publication

Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.
Dehnhardt CM, Venkatesan AM, Chen Z, Ayral-Kaloustian S, Dos Santos O, Delos Santos E, Curran K, Follettie MT, Diesl V, Lucas J, Geng Y, Dejoy SQ, Petersen R, Chaudhary I, Brooijmans N, Mansour TS, Arndt K, Chen L.
J Med Chem (2010) 53 : 897 -910
PubMed 20025292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.07 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL583050 1 6.48
CHEMBL569230 1 6.47
CHEMBL569321 1 6.46
CHEMBL570194 1 6.43
CHEMBL577512 1 6.41
CHEMBL569962 1 6.39
CHEMBL569231 1 6.37
CHEMBL569102 1 6.37
CHEMBL568799 1 6.33
CHEMBL569004 1 6.30
CHEMBL568800 1 6.28
CHEMBL569919 1 6.25
CHEMBL577072 1 6.24
CHEMBL568851 1 6.23
CHEMBL568852 1 6.21
CHEMBL570902 1 6.19
CHEMBL583242 1 6.19
CHEMBL569745 1 6.18
CHEMBL569077 1 6.18
CHEMBL569103 1 6.16
CHEMBL569098 1 6.09
CHEMBL569532 1 6.08
CHEMBL568853 1 6.08
CHEMBL569533 1 6.07
CHEMBL583544 1 6.05
CHEMBL569754 1 6.03
CHEMBL568825 1 6.00
CHEMBL569099 1 5.98
CHEMBL570656 1 5.95
CHEMBL570417 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL583050 IC50 = 329.0 nM 6.48
CHEMBL569230 IC50 = 337.0 nM 6.47
CHEMBL569321 IC50 = 348.0 nM 6.46
CHEMBL570194 IC50 = 374.0 nM 6.43
CHEMBL577512 IC50 = 389.0 nM 6.41
CHEMBL569962 IC50 = 405.0 nM 6.39
CHEMBL569231 IC50 = 431.0 nM 6.37
CHEMBL569102 IC50 = 424.0 nM 6.37
CHEMBL568799 IC50 = 469.0 nM 6.33
CHEMBL569004 IC50 = 506.0 nM 6.30
CHEMBL568800 IC50 = 524.0 nM 6.28
CHEMBL569919 IC50 = 561.0 nM 6.25
CHEMBL577072 IC50 = 573.0 nM 6.24
CHEMBL568851 IC50 = 593.0 nM 6.23
CHEMBL568852 IC50 = 620.0 nM 6.21
CHEMBL570902 IC50 = 645.0 nM 6.19
CHEMBL583242 IC50 = 650.0 nM 6.19
CHEMBL569745 IC50 = 662.0 nM 6.18
CHEMBL569077 IC50 = 659.0 nM 6.18
CHEMBL569103 IC50 = 690.0 nM 6.16
CHEMBL569098 IC50 = 811.0 nM 6.09
CHEMBL568853 IC50 = 840.0 nM 6.08
CHEMBL569532 IC50 = 829.0 nM 6.08
CHEMBL569533 IC50 = 848.0 nM 6.07
CHEMBL583544 IC50 = 895.0 nM 6.05
CHEMBL569754 IC50 = 931.0 nM 6.03
CHEMBL568825 IC50 = 1008.0 nM 6.00
CHEMBL569099 IC50 = 1046.0 nM 5.98
CHEMBL570656 IC50 = 1113.0 nM 5.95
CHEMBL570417 IC50 = 1120.0 nM 5.95
CHEMBL571994 IC50 = 1188.0 nM 5.92
CHEMBL584735 IC50 = 1716.0 nM 5.76
CHEMBL569002 IC50 = 1779.0 nM 5.75
CHEMBL585143 IC50 = 2012.0 nM 5.70
CHEMBL583471 IC50 = 2138.0 nM 5.67
CHEMBL570418 IC50 = 2274.0 nM 5.64
CHEMBL568821 IC50 = 2592.0 nM 5.59
CHEMBL576864 IC50 = 5642.0 nM 5.25
CHEMBL569682 IC50 = 6814.0 nM 5.17
CHEMBL568823 IC50 > 25158.0 nM -
CHEMBL582809 IC50 > 2720.0 nM -