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Assay Detail

CHEMBL981407

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

Binding
Inhibition of Flt3
5
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and development of aurora kinase inhibitors as anticancer agents.
Pollard JR, Mortimore M.
J Med Chem (2009) 52 : 2629 -2651
PubMed 19320489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.86 8.52
Ki 1 7.52 7.52
Kd 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482968 ENMD-2076 2.0 1 8.52
CHEMBL415049 BARASERTIB 3.0 1 8.10
CHEMBL495727 AT-9283 2.0 1 8.00
CHEMBL572878 TOZASERTIB 2.0 1 7.52
CHEMBL482967 CYC-116 1.0 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482968 ENMD-2076 IC50 = 3.0 nM 8.52
CHEMBL415049 BARASERTIB Kd = 8.0 nM 8.10
CHEMBL495727 AT-9283 IC50 = 10.0 nM 8.00
CHEMBL572878 TOZASERTIB Ki = 30.0 nM 7.52
CHEMBL482967 CYC-116 IC50 = 88.0 nM 7.06