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Assay Detail

CHEMBL2327339

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

Binding
Inhibition of JAK2 in human UT7 cells assessed as inhibition of Epo-dependent STAT5 phosphorylation
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type UT7
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
EC50 10 5.39 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322136 1 6.05
CHEMBL2322137 1 5.80
CHEMBL2322134 1 5.55
CHEMBL2322135 1 5.38
CHEMBL2322142 1 5.32
CHEMBL2159198 1 5.18
CHEMBL2322138 1 5.01
CHEMBL2322141 1 4.80
CHEMBL2322143 1 -
CHEMBL2322139 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322136 EC50 = 890.0 nM 6.05
CHEMBL2322137 EC50 = 1600.0 nM 5.80
CHEMBL2322134 EC50 = 2800.0 nM 5.55
CHEMBL2322135 EC50 = 4200.0 nM 5.38
CHEMBL2322142 EC50 = 4800.0 nM 5.32
CHEMBL2159198 EC50 = 6600.0 nM 5.18
CHEMBL2322138 EC50 = 9800.0 nM 5.01
CHEMBL2322141 EC50 = 15800.0 nM 4.80
CHEMBL2322143 EC50 > 20000.0 nM -
CHEMBL2322139 EC50 > 20000.0 nM -