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Assay Detail

CHEMBL5125912

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Binding
Binding affinity to BRD4-T (unknown origin)
8
Total Activities
8
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

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bivalent BET Bromodomain Inhibitors Confer Increased Potency and Selectivity for BRDT via Protein Conformational Plasticity.
Guan X, Cheryala N, Karim RM, Chan A, Berndt N, Qi J, Georg GI, Schönbrunn E.
J Med Chem (2022) 65 : 10441 -10458
PubMed 35867655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.65 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5170488 1 9.54
CHEMBL5206426 1 8.80
CHEMBL5188470 1 8.77
CHEMBL5184876 1 8.64
CHEMBL5178175 1 8.55
CHEMBL5201173 1 8.44
CHEMBL5204093 1 8.32
CHEMBL4760892 1 8.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5170488 Kd = 0.29 nM 9.54
CHEMBL5206426 Kd = 1.6 nM 8.80
CHEMBL5188470 Kd = 1.7 nM 8.77
CHEMBL5184876 Kd = 2.3 nM 8.64
CHEMBL5178175 Kd = 2.8 nM 8.55
CHEMBL5201173 Kd = 3.6 nM 8.44
CHEMBL5204093 Kd = 4.8 nM 8.32
CHEMBL4760892 Kd = 6.7 nM 8.17