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Assay Detail

CHEMBL1954565

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Binding
Inhibition of FLT3
13
Total Activities
13
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

Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.
Pastor J, Oyarzabal J, Saluste G, Alvarez RM, Rivero V, Ramos F, Cendón E, Blanco-Aparicio C, Ajenjo N, Cebriá A, Albarrán MI, Cebrián D, Corrionero A, Fominaya J, Montoya G, Mazzorana M.
Bioorg Med Chem Lett (2012) 22 : 1591 -1597
PubMed 22266039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.62 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1952126 1 7.92
CHEMBL1952136 1 7.55
CHEMBL1952141 1 7.36
CHEMBL1952144 1 6.90
CHEMBL1952113 1 6.64
CHEMBL1952137 1 6.50
CHEMBL1952125 1 6.11
CHEMBL1952142 1 5.40
CHEMBL1952143 1 5.16
CHEMBL1952121 1 -
CHEMBL1952132 1 -
CHEMBL1952133 1 -
CHEMBL1952134 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1952126 IC50 = 12.0 nM 7.92
CHEMBL1952136 IC50 = 28.0 nM 7.55
CHEMBL1952141 IC50 = 44.0 nM 7.36
CHEMBL1952144 IC50 = 125.0 nM 6.90
CHEMBL1952113 IC50 = 231.0 nM 6.64
CHEMBL1952137 IC50 = 314.0 nM 6.50
CHEMBL1952125 IC50 = 778.0 nM 6.11
CHEMBL1952142 IC50 = 4000.0 nM 5.40
CHEMBL1952143 IC50 = 7000.0 nM 5.16
CHEMBL1952121 IC50 > 1000.0 nM -
CHEMBL1952132 IC50 > 1000.0 nM -
CHEMBL1952133 IC50 > 1000.0 nM -
CHEMBL1952134 IC50 > 1000.0 nM -