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Assay Detail

CHEMBL1106056

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Binding
Inhibition of FLT3 by HTRF assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells.
Choi SJ, Moon MJ, Lee SD, Choi SU, Han SY, Kim YC.
Bioorg Med Chem Lett (2010) 20 : 2033 -2037
PubMed 20153646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.84 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603469 LESTAURTINIB 3.0 1 8.30
CHEMBL1095687 1 8.05
CHEMBL1077291 1 7.82
CHEMBL1097359 1 7.55
CHEMBL126077 INDIRUBIN-3-MONOXIME 1 7.48
CHEMBL369303 1 7.21
CHEMBL511450 1 7.09
CHEMBL604263 1 6.89
CHEMBL111433 1 6.68
CHEMBL367113 1 6.67
CHEMBL368689 1 6.55
CHEMBL594192 1 6.45
CHEMBL337300 1 6.38
CHEMBL1095374 1 6.02
CHEMBL173445 1 5.33
CHEMBL367345 1 5.00
CHEMBL1085921 1 -
CHEMBL174025 1 -
CHEMBL1276127 INDIRUBIN 2.0 1 -
CHEMBL1083839 1 -
CHEMBL1095686 1 -
CHEMBL1086983 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603469 LESTAURTINIB IC50 = 5.0 nM 8.30
CHEMBL1095687 IC50 = 9.0 nM 8.05
CHEMBL1077291 IC50 = 15.0 nM 7.82
CHEMBL1097359 IC50 = 28.0 nM 7.55
CHEMBL126077 INDIRUBIN-3-MONOXIME IC50 = 33.0 nM 7.48
CHEMBL369303 IC50 = 62.0 nM 7.21
CHEMBL511450 IC50 = 82.0 nM 7.09
CHEMBL604263 IC50 = 128.0 nM 6.89
CHEMBL111433 IC50 = 209.0 nM 6.68
CHEMBL367113 IC50 = 212.0 nM 6.67
CHEMBL368689 IC50 = 280.0 nM 6.55
CHEMBL594192 IC50 = 359.0 nM 6.45
CHEMBL337300 IC50 = 418.0 nM 6.38
CHEMBL1095374 IC50 = 952.0 nM 6.02
CHEMBL173445 IC50 = 4722.0 nM 5.33
CHEMBL367345 IC50 = 10070.0 nM 5.00
CHEMBL1085921 IC50 > 10000.0 nM -
CHEMBL174025 IC50 > 10000.0 nM -
CHEMBL1276127 INDIRUBIN IC50 > 10000.0 nM -
CHEMBL1083839 IC50 > 10000.0 nM -
CHEMBL1095686 IC50 > 10000.0 nM -
CHEMBL1086983 IC50 > 10000.0 nM -