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Assay Detail

CHEMBL4155885

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Binding
Inhibition of human FLT3 by Hotspot assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of the selective and efficacious inhibitors of FLT3 mutations.
Zhi Y, Li B, Yao C, Li H, Chen P, Bao J, Qin T, Wang Y, Lu T, Lu S.
Eur J Med Chem (2018) 155 : 303 -315
PubMed 29894944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.73 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4163870 1 9.72
CHEMBL4172223 1 9.33
CHEMBL4075720 1 9.22
CHEMBL4164331 1 9.21
CHEMBL4175865 1 9.19
CHEMBL4171138 1 9.18
CHEMBL4159478 1 9.18
CHEMBL4160544 1 9.14
CHEMBL4160930 1 9.02
CHEMBL388978 STAUROSPORINE 1 8.82
CHEMBL4172658 1 8.60
CHEMBL4162003 1 8.47
CHEMBL4168002 1 8.44
CHEMBL4168869 1 8.42
CHEMBL4167321 1 7.95
CHEMBL4167778 1 7.80
CHEMBL4175644 1 7.78
CHEMBL4159414 1 7.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4163870 IC50 = 0.19 nM 9.72
CHEMBL4172223 IC50 = 0.47 nM 9.33
CHEMBL4075720 IC50 = 0.6 nM 9.22
CHEMBL4164331 IC50 = 0.62 nM 9.21
CHEMBL4175865 IC50 = 0.65 nM 9.19
CHEMBL4171138 IC50 = 0.66 nM 9.18
CHEMBL4159478 IC50 = 0.66 nM 9.18
CHEMBL4160544 IC50 = 0.73 nM 9.14
CHEMBL4160930 IC50 = 0.95 nM 9.02
CHEMBL388978 STAUROSPORINE IC50 = 1.52 nM 8.82
CHEMBL4172658 IC50 = 2.53 nM 8.60
CHEMBL4162003 IC50 = 3.42 nM 8.47
CHEMBL4168002 IC50 = 3.63 nM 8.44
CHEMBL4168869 IC50 = 3.8 nM 8.42
CHEMBL4167321 IC50 = 11.31 nM 7.95
CHEMBL4167778 IC50 = 15.7 nM 7.80
CHEMBL4175644 IC50 = 16.5 nM 7.78
CHEMBL4159414 IC50 = 20.51 nM 7.69