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Assay Detail

CHEMBL4340980

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

Binding
Inhibition of human FLT3 using EAIYAAPFAKKK as substrate incubated for 60 mins by fluorescence based assay
13
Total Activities
13
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 novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J.
Eur J Med Chem (2019) 168 : 87 -109
PubMed 30802730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.91 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1952329 SGI-1776 1.0 1 7.68
CHEMBL4527736 1 5.40
CHEMBL1952142 1 5.36
CHEMBL4526558 1 5.20
CHEMBL4468395 1 -
CHEMBL4543342 1 -
CHEMBL4576509 1 -
CHEMBL4547383 1 -
CHEMBL4556293 1 -
CHEMBL4483071 1 -
CHEMBL4460019 1 -
CHEMBL4521827 1 -
CHEMBL4449598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1952329 SGI-1776 IC50 = 21.0 nM 7.68
CHEMBL4527736 IC50 = 3970.0 nM 5.40
CHEMBL1952142 IC50 = 4350.0 nM 5.36
CHEMBL4526558 IC50 = 6320.0 nM 5.20
CHEMBL4468395 IC50 > 10000.0 nM -
CHEMBL4543342 IC50 > 10000.0 nM -
CHEMBL4576509 IC50 > 10000.0 nM -
CHEMBL4547383 IC50 > 10000.0 nM -
CHEMBL4556293 IC50 > 10000.0 nM -
CHEMBL4483071 IC50 > 10000.0 nM -
CHEMBL4460019 IC50 > 10000.0 nM -
CHEMBL4521827 IC50 > 10000.0 nM -
CHEMBL4449598 IC50 > 10000.0 nM -