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Assay Detail

CHEMBL2050054

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

Functional
Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Autocuration

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo.
Li WW, Wang XY, Zheng RL, Yan HX, Cao ZX, Zhong L, Wang ZR, Ji P, Yang LL, Wang LJ, Xu Y, Liu JJ, Yang J, Zhang CH, Ma S, Feng S, Sun QZ, Wei YQ, Yang SY.
J Med Chem (2012) 55 : 3852 -3866
PubMed 22452518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.54 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2046884 1 9.52
CHEMBL535 SUNITINIB 4.0 1 8.52
CHEMBL2046733 1 8.30
CHEMBL2046883 1 8.22
CHEMBL2046882 1 8.00
CHEMBL2046448 1 7.92
CHEMBL2046730 1 7.70
CHEMBL2046713 1 7.70
CHEMBL2046732 1 7.66
CHEMBL2046879 1 7.66
CHEMBL2046717 1 7.60
CHEMBL2046718 1 7.57
CHEMBL124660 TANDUTINIB 2.0 1 7.26
CHEMBL2046716 1 6.68
CHEMBL2046880 1 6.52
CHEMBL2046731 1 6.40
CHEMBL2046711 1 6.35
CHEMBL2046719 1 6.20
CHEMBL2046723 1 6.08
CHEMBL2046704 1 5.99
CHEMBL2046703 1 5.95
CHEMBL2046708 1 5.94
CHEMBL2046699 1 5.94
CHEMBL2046726 1 5.92
CHEMBL2046702 1 5.91
CHEMBL2046727 1 5.87
CHEMBL2046712 1 5.85
CHEMBL2046709 1 5.85
CHEMBL2046705 1 5.82
CHEMBL2046707 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2046884 IC50 = 0.3 nM 9.52
CHEMBL535 SUNITINIB IC50 = 3.0 nM 8.52
CHEMBL2046733 IC50 = 5.0 nM 8.30
CHEMBL2046883 IC50 = 6.0 nM 8.22
CHEMBL2046882 IC50 = 10.0 nM 8.00
CHEMBL2046448 IC50 = 12.0 nM 7.92
CHEMBL2046730 IC50 = 20.0 nM 7.70
CHEMBL2046713 IC50 = 20.0 nM 7.70
CHEMBL2046732 IC50 = 22.0 nM 7.66
CHEMBL2046879 IC50 = 22.0 nM 7.66
CHEMBL2046717 IC50 = 25.0 nM 7.60
CHEMBL2046718 IC50 = 27.0 nM 7.57
CHEMBL124660 TANDUTINIB IC50 = 55.0 nM 7.26
CHEMBL2046716 IC50 = 210.0 nM 6.68
CHEMBL2046880 IC50 = 300.0 nM 6.52
CHEMBL2046731 IC50 = 400.0 nM 6.40
CHEMBL2046711 IC50 = 450.0 nM 6.35
CHEMBL2046719 IC50 = 625.0 nM 6.20
CHEMBL2046723 IC50 = 830.0 nM 6.08
CHEMBL2046704 IC50 = 1020.0 nM 5.99
CHEMBL2046703 IC50 = 1130.0 nM 5.95
CHEMBL2046699 IC50 = 1140.0 nM 5.94
CHEMBL2046708 IC50 = 1150.0 nM 5.94
CHEMBL2046726 IC50 = 1200.0 nM 5.92
CHEMBL2046702 IC50 = 1240.0 nM 5.91
CHEMBL2046727 IC50 = 1350.0 nM 5.87
CHEMBL2046712 IC50 = 1400.0 nM 5.85
CHEMBL2046709 IC50 = 1400.0 nM 5.85
CHEMBL2046705 IC50 = 1500.0 nM 5.82
CHEMBL2046707 IC50 = 1600.0 nM 5.80
CHEMBL2046700 IC50 = 1610.0 nM 5.79
CHEMBL2046721 IC50 = 1900.0 nM 5.72
CHEMBL2046720 IC50 = 2420.0 nM 5.62
CHEMBL2046724 IC50 = 2880.0 nM 5.54
CHEMBL2046701 IC50 = 2950.0 nM 5.53
CHEMBL2046706 IC50 = 3000.0 nM 5.52
CHEMBL2046722 IC50 = 3200.0 nM 5.50
CHEMBL2046710 IC50 = 3680.0 nM 5.43
CHEMBL2046881 IC50 = 6000.0 nM 5.22
CHEMBL2046725 IC50 = 9040.0 nM 5.04
CHEMBL2046729 IC50 > 10000.0 nM -
CHEMBL2046728 IC50 > 11000.0 nM -
CHEMBL2046715 IC50 > 10000.0 nM -
CHEMBL2046714 IC50 > 5000.0 nM -