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Assay Detail

CHEMBL5120719

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

Binding
Protac activity at E3 ubiquitin ligase/JAK2 in human MHH-CALL-4 cells assessed as E3 ubiquitin ligase mediated JAK2 degradation incubated for 32 hrs by immunoblotting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MHHCALL4
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Potent PROTACs for the Potential Treatment of Leukemia.
Kargbo RB.
ACS Med Chem Lett (2022) 13 : 1831 -1832
PubMed 36518705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.43 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741262 1 9.70
CHEMBL5195930 1 9.30
CHEMBL4790924 1 9.30
CHEMBL4742130 1 9.27
CHEMBL4789389 1 9.05
CHEMBL4759504 1 8.57
CHEMBL4784942 1 8.41
CHEMBL4764854 1 7.82
CHEMBL4744617 1 6.91
CHEMBL4781392 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741262 EC50 = 0.2 nM 9.70
CHEMBL5195930 EC50 = 0.5 nM 9.30
CHEMBL4790924 EC50 = 0.5 nM 9.30
CHEMBL4742130 EC50 = 0.54 nM 9.27
CHEMBL4789389 EC50 = 0.9 nM 9.05
CHEMBL4759504 EC50 = 2.7 nM 8.57
CHEMBL4784942 EC50 = 3.9 nM 8.41
CHEMBL4764854 EC50 = 15.0 nM 7.82
CHEMBL4744617 EC50 = 122.0 nM 6.91
CHEMBL4781392 EC50 = 1100.0 nM 5.96