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Assay Detail

CHEMBL5317223

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Binding
Binding affinity to YEATS4 (unknown origin) assessed as dissociation constant by isothermal calorimetric analysis
5
Total Activities
5
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

YEATS domain-containing protein 4 (CHEMBL4296266)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
Londregan AT, Aitmakhanova K, Bennett J, Byrnes LJ, Canterbury DP, Cheng X, Christott T, Clemens J, Coffey SB, Dias JM, Dowling MS, Farnie G, Fedorov O, Fennell KF, Gamble V, Gileadi C, Giroud C, Harris MR, Hollingshead BD, Huber K, Korczynska M, Lapham K, Loria PM, Narayanan A, Owen DR, Raux B, Sahasrabudhe PV, Ruggeri RB, Sáez LD, Stock IA, Thuma BA, Tsai A, Varghese AE.
J Med Chem (2023) 66 : 460 -472
PubMed 36562986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.31 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439842 1 7.52
CHEMBL5434894 1 7.35
CHEMBL5397585 1 7.28
CHEMBL5428051 1 7.28
CHEMBL5411016 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439842 Kd = 30.0 nM 7.52
CHEMBL5434894 Kd = 45.0 nM 7.35
CHEMBL5397585 Kd = 53.0 nM 7.28
CHEMBL5428051 Kd = 52.7 nM 7.28
CHEMBL5411016 Kd = 80.0 nM 7.10