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Assay Detail

CHEMBL2327181

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

Binding
Inhibition of JAK2 (unknown origin) after 2.5 hrs by time-resolved fluorescence resonance energy transfer assay in presence of 100 uM ATP
3
Total Activities
3
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

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

Publication

Design and synthesis of tricyclic cores for kinase inhibition.
Van Epps S, Fiamengo B, Edmunds J, Ericsson A, Frank K, Friedman M, George D, George J, Goedken E, Kotecki B, Martinez G, Merta P, Morytko M, Shekhar S, Skinner B, Stewart K, Voss J, Wallace G, Wang L, Wang L, Wishart N.
Bioorg Med Chem Lett (2013) 23 : 693 -698
PubMed 23265875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.13 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322138 1 5.24
CHEMBL2159198 1 5.22
CHEMBL2322139 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322138 IC50 = 5700.0 nM 5.24
CHEMBL2159198 IC50 = 6000.0 nM 5.22
CHEMBL2322139 IC50 = 11400.0 nM 4.94