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Assay Detail

CHEMBL5708845

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

Binding
Inhibition of recombinant N-terminal GST-tagged FLT3 (unknown origin) expressed in Bac-to-Bac baculovirus expression system incubated for 2 hrs using poly(Glu,Tyr) as substrate in presence of ATP by multi-label plate reader analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
4
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

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies.
Hart S, Goh KC, Novotny-Diermayr V, Hu CY, Hentze H, Tan YC, Madan B, Amalini C, Loh YK, Ong LC, William AD, Lee A, Poulsen A, Jayaraman R, Ong KH, Ethirajulu K, Dymock BW, Wood JW.
Leukemia (2011) 25 : 1751 -1759
PubMed 21691275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.66 7.66

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000574
EFO_ID EFO_ID - HP:0011974
EFO_TERM EFO_TERM - lymphoma
EFO_TERM EFO_TERM - myelofibrosis

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035187 PACRITINIB 4.0 1 7.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035187 PACRITINIB IC50 = 22.0 nM 7.66