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Assay Detail

CHEMBL4739212

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Binding
Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR analysis
10
Total Activities
10
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

Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
O' Donovan DH,Gregson C,Packer MJ,Greenwood R,Pike KG,Kawatkar S,Bloecher A,Robinson J,Read J,Code E,Hsu JH,Shen M,Woods H,Barton P,Fillery S,Williamson B,Rawlins PB,Bagal SK
Bioorg Med Chem Lett (2021) 39 : 127904 -127904
PubMed 33684441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 5.81 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755618 1 6.40
CHEMBL4759335 1 6.30
CHEMBL4754048 1 5.92
CHEMBL4762963 1 5.62
CHEMBL4748924 1 4.82
CHEMBL4785927 1 -
CHEMBL4752420 1 -
CHEMBL4792277 1 -
CHEMBL4751508 1 -
CHEMBL4763811 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755618 Kd = 400.0 nM 6.40
CHEMBL4759335 Kd = 500.0 nM 6.30
CHEMBL4754048 Kd = 1200.0 nM 5.92
CHEMBL4762963 Kd = 2400.0 nM 5.62
CHEMBL4748924 Kd = 15000.0 nM 4.82
CHEMBL4785927 Kd - -
CHEMBL4752420 Kd = 305000.0 nM -
CHEMBL4792277 Kd - -
CHEMBL4751508 Kd - -
CHEMBL4763811 Kd - -