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Assay Detail

CHEMBL5519283

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

Binding
Binding affinity to PELI1 FHA domain (unknown origin) expressed in Escherichia coli BL21(DE3) competent cell measured after 1 min by fluorescence quenching assay
54
Total Activities
54
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

E3 ubiquitin-protein ligase pellino homolog 1 (CHEMBL6066217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Resveratrol-derived inhibitors of the E3 ubiquitin ligase PELI1 inhibit the metastasis of triple-negative breast cancer.
Xu G, Zhou Q, Qi J, Li Z, Yin L, Li Z, Lu C, Zhao B, Shen Y.
Eur J Med Chem (2024) 265 : 116060 -116060
PubMed 38150964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 54 4.53 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5560298 1 5.28
CHEMBL5542921 1 5.24
CHEMBL5566406 1 5.15
CHEMBL5412968 1 5.09
CHEMBL5562660 1 4.94
CHEMBL5559040 1 4.92
CHEMBL5410440 1 4.87
CHEMBL5440044 1 4.82
CHEMBL5432112 1 4.71
CHEMBL5435393 1 4.65
CHEMBL5417329 1 4.58
CHEMBL5418959 1 4.57
CHEMBL5403221 1 4.42
CHEMBL5560896 1 4.41
CHEMBL5558789 1 4.40
CHEMBL5415636 1 4.37
CHEMBL5404281 1 4.37
CHEMBL5424509 1 4.35
CHEMBL5557659 1 4.29
CHEMBL5395090 1 4.28
CHEMBL5401135 1 4.25
CHEMBL5395132 1 4.22
CHEMBL5428405 1 4.19
CHEMBL5567921 1 4.15
CHEMBL5557050 1 4.09
CHEMBL5557824 1 4.06
CHEMBL5398839 1 4.05
CHEMBL5560444 1 4.02
CHEMBL5398320 1 -
CHEMBL5437018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5560298 Kd = 5200.0 nM 5.28
CHEMBL5542921 Kd = 5800.0 nM 5.24
CHEMBL5566406 Kd = 7100.0 nM 5.15
CHEMBL5412968 Kd = 8200.0 nM 5.09
CHEMBL5562660 Kd = 11400.0 nM 4.94
CHEMBL5559040 Kd = 11900.0 nM 4.92
CHEMBL5410440 Kd = 13620.0 nM 4.87
CHEMBL5440044 Kd = 15300.0 nM 4.82
CHEMBL5432112 Kd = 19720.0 nM 4.71
CHEMBL5435393 Kd = 22600.0 nM 4.65
CHEMBL5417329 Kd = 26300.0 nM 4.58
CHEMBL5418959 Kd = 26900.0 nM 4.57
CHEMBL5403221 Kd = 37900.0 nM 4.42
CHEMBL5560896 Kd = 39300.0 nM 4.41
CHEMBL5558789 Kd = 40100.0 nM 4.40
CHEMBL5415636 Kd = 43200.0 nM 4.37
CHEMBL5404281 Kd = 42300.0 nM 4.37
CHEMBL5424509 Kd = 44400.0 nM 4.35
CHEMBL5557659 Kd = 51500.0 nM 4.29
CHEMBL5395090 Kd = 52180.0 nM 4.28
CHEMBL5401135 Kd = 55700.0 nM 4.25
CHEMBL5395132 Kd = 59900.0 nM 4.22
CHEMBL5428405 Kd = 64300.0 nM 4.19
CHEMBL5567921 Kd = 70100.0 nM 4.15
CHEMBL5557050 Kd = 80600.0 nM 4.09
CHEMBL5557824 Kd = 86900.0 nM 4.06
CHEMBL5398839 Kd = 89100.0 nM 4.05
CHEMBL5560444 Kd = 96300.0 nM 4.02
CHEMBL5430291 Kd = 130700.0 nM -
CHEMBL5558025 Kd = 103700.0 nM -
CHEMBL5412740 Kd - -
CHEMBL5425612 Kd - -
CHEMBL5403522 Kd - -
CHEMBL5438701 Kd - -
CHEMBL5404654 Kd - -
CHEMBL5408248 Kd - -
CHEMBL5424388 Kd - -
CHEMBL165 RESVERATROL Kd = 125300.0 nM -
CHEMBL244948 DAPHNETIN Kd = 336000.0 nM -
CHEMBL13883 VANILLIN Kd = 227500.0 nM -
CHEMBL1797870 Kd = 211900.0 nM -
CHEMBL454533 NICOTINANILIDE Kd = 336000.0 nM -
CHEMBL2136039 Kd = 297900.0 nM -
CHEMBL5418790 Kd - -
CHEMBL5419187 Kd - -
CHEMBL5409654 Kd - -
CHEMBL5421402 Kd - -
CHEMBL5423037 Kd - -
CHEMBL5437018 Kd - -
CHEMBL5398320 Kd - -