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Assay Detail

CHEMBL2183761

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

Binding
Inhibition of JAK2 V617F mutant expressed in mouse Ba/f3 cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET, Goh KC, Ong WC, Goh SK, Hart S, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW.
J Med Chem (2011) 54 : 4638 -4658
PubMed 21604762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.72 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2035187 PACRITINIB 4.0 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2035187 PACRITINIB IC50 = 19.0 nM 7.72