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Assay Detail

CHEMBL4059046

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

Binding
Binding affinity to human full length recombinant His-tagged HuR expressed in Escherichia coli Rosetta DH5alpha assessed as inhibition of interaction with single-strand Bi-AU RNA probe by AlphaScreen assay
17
Total Activities
17
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

ELAV-like protein 1 (CHEMBL1250379)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interfering with HuR-RNA Interaction: Design, Synthesis and Biological Characterization of Tanshinone Mimics as Novel, Effective HuR Inhibitors.
Manzoni L, Zucal C, Maio DD, D'Agostino VG, Thongon N, Bonomo I, Lal P, Miceli M, Baj V, Brambilla M, Cerofolini L, Elezgarai S, Biasini E, Luchinat C, Novellino E, Fragai M, Marinelli L, Provenzani A, Seneci P.
J Med Chem (2018) 61 : 1483 -1498
PubMed 29313684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.42 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075458 1 7.89
CHEMBL4064932 1 7.82
CHEMBL4095060 1 7.39
CHEMBL4100171 1 7.32
CHEMBL227075 DIHYDROTANSHINONE I 1 7.30
CHEMBL4105230 1 7.26
CHEMBL4073526 1 7.25
CHEMBL4094161 1 7.09
CHEMBL4067653 1 -
CHEMBL4102819 1 -
CHEMBL4092808 1 -
CHEMBL4081086 1 -
CHEMBL4075620 1 -
CHEMBL4077265 1 -
CHEMBL4076484 1 -
CHEMBL4070465 1 -
CHEMBL4073683 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075458 Ki = 12.8 nM 7.89
CHEMBL4064932 Ki = 15.0 nM 7.82
CHEMBL4095060 Ki = 41.0 nM 7.39
CHEMBL4100171 Ki = 48.0 nM 7.32
CHEMBL227075 DIHYDROTANSHINONE I Ki = 50.0 nM 7.30
CHEMBL4105230 Ki = 55.0 nM 7.26
CHEMBL4073526 Ki = 56.0 nM 7.25
CHEMBL4094161 Ki = 81.0 nM 7.09
CHEMBL4067653 Ki > 100.0 nM -
CHEMBL4102819 Ki > 100.0 nM -
CHEMBL4092808 Ki > 100.0 nM -
CHEMBL4081086 Ki > 100.0 nM -
CHEMBL4075620 Ki > 200.0 nM -
CHEMBL4077265 Ki > 200.0 nM -
CHEMBL4076484 Ki > 100.0 nM -
CHEMBL4070465 Ki > 200.0 nM -
CHEMBL4073683 Ki > 300.0 nM -