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Assay Detail

CHEMBL5317208

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

Binding
Binding affinity to human his-tagged recombinant YEATS4 expressed in Escherichia coli assessed as inhibition constant using biotin tagged lysine 27-crotonylated histone H3 peptide as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by FRET analysis
13
Total Activities
13
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
Ki 13 7.17 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397585 1 7.68
CHEMBL5414722 1 7.48
CHEMBL5428051 1 7.48
CHEMBL5439842 1 7.43
CHEMBL5432565 1 7.37
CHEMBL5439506 1 7.25
CHEMBL5426169 1 7.24
CHEMBL5434894 1 7.23
CHEMBL5411016 1 7.20
CHEMBL5432083 1 7.16
CHEMBL5429949 1 6.85
CHEMBL5435884 1 6.55
CHEMBL5439514 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397585 Ki = 21.0 nM 7.68
CHEMBL5414722 Ki = 33.0 nM 7.48
CHEMBL5428051 Ki = 33.0 nM 7.48
CHEMBL5439842 Ki = 37.0 nM 7.43
CHEMBL5432565 Ki = 43.0 nM 7.37
CHEMBL5439506 Ki = 56.0 nM 7.25
CHEMBL5426169 Ki = 57.0 nM 7.24
CHEMBL5434894 Ki = 59.0 nM 7.23
CHEMBL5411016 Ki = 63.0 nM 7.20
CHEMBL5432083 Ki = 69.0 nM 7.16
CHEMBL5429949 Ki = 141.0 nM 6.85
CHEMBL5435884 Ki = 284.0 nM 6.55
CHEMBL5439514 Ki = 540.0 nM 6.27