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Assay Detail

CHEMBL3405277

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

Binding
Inhibition of FLT3 (unknown origin)
17
Total Activities
17
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

Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors.
Boyd MJ, Bandarage UK, Bennett H, Byrn RR, Davies I, Gu W, Jacobs M, Ledeboer MW, Ledford B, Leeman JR, Perola E, Wang T, Bennani Y, Clark MP, Charifson PS.
Bioorg Med Chem Lett (2015) 25 : 1990 -1994
PubMed 25827523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.08 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3401987 1 6.82
CHEMBL3401984 1 6.80
CHEMBL3401978 1 6.68
CHEMBL3401979 1 6.10
CHEMBL3401990 1 6.08
CHEMBL3401988 1 6.01
CHEMBL3401976 1 5.96
CHEMBL3401983 1 5.92
CHEMBL3401986 1 5.85
CHEMBL3401989 1 5.75
CHEMBL3401980 1 5.55
CHEMBL3401985 1 5.40
CHEMBL3401982 1 -
CHEMBL3318007 PIMODIVIR 3.0 1 -
CHEMBL3401981 1 -
CHEMBL3401977 1 -
CHEMBL3401975 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3401987 Ki = 150.0 nM 6.82
CHEMBL3401984 Ki = 160.0 nM 6.80
CHEMBL3401978 Ki = 210.0 nM 6.68
CHEMBL3401979 Ki = 800.0 nM 6.10
CHEMBL3401990 Ki = 840.0 nM 6.08
CHEMBL3401988 Ki = 970.0 nM 6.01
CHEMBL3401976 Ki = 1100.0 nM 5.96
CHEMBL3401983 Ki = 1200.0 nM 5.92
CHEMBL3401986 Ki = 1400.0 nM 5.85
CHEMBL3401989 Ki = 1800.0 nM 5.75
CHEMBL3401980 Ki = 2800.0 nM 5.55
CHEMBL3401985 Ki = 4000.0 nM 5.40
CHEMBL3401982 Ki > 4000.0 nM -
CHEMBL3318007 PIMODIVIR Ki > 4000.0 nM -
CHEMBL3401981 Ki > 4000.0 nM -
CHEMBL3401977 Ki > 4000.0 nM -
CHEMBL3401975 Ki > 4000.0 nM -