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Assay Detail

CHEMBL4020043

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

Binding
Binding affinity to His tagged human EED (77 to 441 residues) expressed in Escherichia coli BL21(DE3)-T1R by ITC method
13
Total Activities
13
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

Polycomb protein EED (CHEMBL2189117)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Are We There Yet? Applying Thermodynamic and Kinetic Profiling on Embryonic Ectoderm Development (EED) Hit-to-Lead Program.
Wang Y, Edalji RP, Panchal SC, Sun C, Djuric SW, Vasudevan A.
J Med Chem (2017) 60 : 8321 -8335
PubMed 28926243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 6.64 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4085428 1 8.22
CHEMBL4084398 1 8.00
CHEMBL4080018 1 8.00
CHEMBL4072980 1 7.52
CHEMBL4075197 1 7.05
CHEMBL4077899 1 6.96
CHEMBL4067115 1 6.43
CHEMBL4093678 1 6.03
CHEMBL4071358 1 5.94
CHEMBL4060827 1 5.68
CHEMBL4092154 1 5.66
CHEMBL4064198 1 5.60
CHEMBL51594 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4085428 Kd = 6.0 nM 8.22
CHEMBL4084398 Kd = 10.0 nM 8.00
CHEMBL4080018 Kd = 10.0 nM 8.00
CHEMBL4072980 Kd = 30.0 nM 7.52
CHEMBL4075197 Kd = 90.0 nM 7.05
CHEMBL4077899 Kd = 110.0 nM 6.96
CHEMBL4067115 Kd = 370.0 nM 6.43
CHEMBL4093678 Kd = 940.0 nM 6.03
CHEMBL4071358 Kd = 1140.0 nM 5.94
CHEMBL4060827 Kd = 2100.0 nM 5.68
CHEMBL4092154 Kd = 2200.0 nM 5.66
CHEMBL4064198 Kd = 2500.0 nM 5.60
CHEMBL51594 Kd = 5200.0 nM 5.28