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Assay Detail

CHEMBL1942933

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Binding
Inhibition of FLT3 phosphorylation by cell based assay
33
Total Activities
33
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

Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
Plé PA, Jung F, Ashton S, Hennequin L, Laine R, Morgentin R, Pasquet G, Taylor S.
Bioorg Med Chem Lett (2012) 22 : 262 -266
PubMed 22153662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 8.11 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940109 1 8.70
CHEMBL1940108 1 8.70
CHEMBL1940107 1 8.52
CHEMBL1940110 1 8.52
CHEMBL1940103 1 8.40
CHEMBL1940105 1 8.40
CHEMBL1940116 1 8.40
CHEMBL1940273 1 8.40
CHEMBL1940268 1 8.30
CHEMBL1940113 1 8.30
CHEMBL1940112 1 8.30
CHEMBL1940274 1 8.15
CHEMBL1940259 1 8.15
CHEMBL1940262 1 8.10
CHEMBL1940118 1 8.05
CHEMBL1940272 1 8.00
CHEMBL1940266 1 8.00
CHEMBL1940106 1 8.00
CHEMBL1940111 1 8.00
CHEMBL1940275 1 7.70
CHEMBL1940269 1 7.70
CHEMBL1940267 1 7.70
CHEMBL1940115 1 7.70
CHEMBL1940114 1 7.40
CHEMBL1940271 1 7.10
CHEMBL1940265 1 -
CHEMBL1940264 1 -
CHEMBL1940263 1 -
CHEMBL1940261 1 -
CHEMBL1940260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940109 IC50 = 2.0 nM 8.70
CHEMBL1940108 IC50 = 2.0 nM 8.70
CHEMBL1940107 IC50 = 3.0 nM 8.52
CHEMBL1940110 IC50 = 3.0 nM 8.52
CHEMBL1940103 IC50 = 4.0 nM 8.40
CHEMBL1940105 IC50 = 4.0 nM 8.40
CHEMBL1940116 IC50 = 4.0 nM 8.40
CHEMBL1940273 IC50 = 4.0 nM 8.40
CHEMBL1940268 IC50 = 5.0 nM 8.30
CHEMBL1940112 IC50 = 5.0 nM 8.30
CHEMBL1940113 IC50 = 5.0 nM 8.30
CHEMBL1940274 IC50 = 7.0 nM 8.15
CHEMBL1940259 IC50 = 7.0 nM 8.15
CHEMBL1940262 IC50 = 8.0 nM 8.10
CHEMBL1940118 IC50 = 9.0 nM 8.05
CHEMBL1940266 IC50 = 10.0 nM 8.00
CHEMBL1940111 IC50 = 10.0 nM 8.00
CHEMBL1940106 IC50 = 10.0 nM 8.00
CHEMBL1940272 IC50 = 10.0 nM 8.00
CHEMBL1940275 IC50 = 20.0 nM 7.70
CHEMBL1940269 IC50 = 20.0 nM 7.70
CHEMBL1940267 IC50 = 20.0 nM 7.70
CHEMBL1940115 IC50 = 20.0 nM 7.70
CHEMBL1940114 IC50 = 40.0 nM 7.40
CHEMBL1940271 IC50 = 80.0 nM 7.10
CHEMBL1940265 IC50 > 400.0 nM -
CHEMBL1940264 IC50 > 1000.0 nM -
CHEMBL1940263 IC50 > 1000.0 nM -
CHEMBL1940261 IC50 > 1000.0 nM -
CHEMBL1940260 IC50 > 60.0 nM -
CHEMBL1940270 IC50 > 800.0 nM -
CHEMBL1940117 IC50 > 1000.0 nM -
CHEMBL1940104 IC50 > 20.0 nM -