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Assay Detail

CHEMBL5348525

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

Binding
Binding affinity to CECR2 (unknown origin) assessed as dissociation constant by site-directed competition binding assay
4
Total Activities
4
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

Chromatin remodeling regulator CECR2 (CHEMBL3108639)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel pan-selective bromodomain inhibitor for epigenetic drug design.
Warstat R, Pervaiz M, Regenass P, Amann M, Schmidtkunz K, Einsle O, Jung M, Breit B, Hügle M, Günther S.
Eur J Med Chem (2023) 249 : 115139 -115139
PubMed 36736153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.06 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3133807 1 8.10
CHEMBL5439294 1 6.01
CHEMBL5398641 1 -
CHEMBL5433870 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3133807 Kd = 8.0 nM 8.10
CHEMBL5439294 Kd = 970.0 nM 6.01
CHEMBL5398641 Kd > 10000.0 nM -
CHEMBL5433870 Kd > 10000.0 nM -