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Assay Detail

CHEMBL5577171

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Binding
Binding affinity to BRDT BD1 (unknown origin) assessed as dissociation constant by BROMOscan assay
3
Total Activities
3
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 testis-specific protein (CHEMBL1795185)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent, orally available furopyridine derivative as a novel selective bromodomain and extra-terminal domain (BET)-first bromodomain (BD1) inhibitor.
Hagihara S, Ishizawa K, Kikuchi M, Kawano Y, Nishidate A, Matsumoto F, Hashimoto N, Sasaki C, Miyaguchi I, Okada O, Akashi T, Nakayama S, Ogasawara Y, Endo J.
Bioorg Med Chem Lett (2024) 109 : 129848 -129848
PubMed 38876176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 8.10 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5590067 1 8.70
CHEMBL5590913 1 8.52
CHEMBL5590578 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5590067 Kd = 2.0 nM 8.70
CHEMBL5590913 Kd = 3.0 nM 8.52
CHEMBL5590578 Kd = 86.0 nM 7.07