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Assay Detail

CHEMBL4679656

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

Binding
Binding affinity to human CRBN-thalidomide binding domain expressed in Escherichia coli by measuring baseline corrected normalized fluorescence by MST based assay
40
Total Activities
24
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein cereblon (CHEMBL3763008)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.
Maiwald S,Heim C,Hernandez Alvarez B,Hartmann MD
ACS Med Chem Lett (2021) 12 : 74 -81
PubMed 33488967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.49 4.81
Ki 16 4.82 5.33
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137312 DASABUVIR 4.0 2 5.33
CHEMBL3989927 IBERDOMIDE 3.0 2 5.31
CHEMBL275661 SUCCINIMIDE -1.0 2 5.09
CHEMBL43452 POMALIDOMIDE 4.0 2 5.00
CHEMBL848 LENALIDOMIDE 4.0 2 4.79
CHEMBL3989934 AVADOMIDE 2.0 2 4.78
CHEMBL4797970 2 4.51
CHEMBL4759876 2 4.39
CHEMBL4758352 2 4.17
CHEMBL100259 URIDINE 3.0 2 -
CHEMBL1259059 SOFOSBUVIR 4.0 1 -
CHEMBL566 URACIL 3.0 2 -
CHEMBL63 ROLIPRAM 2.0 2 -
CHEMBL504 DIMETHYL SULFOXIDE 4.0 2 -
CHEMBL214393 1 -
CHEMBL122334 HYDANTOIN 2 -
CHEMBL30446 1 -
CHEMBL3707254 FURAZIDIN -1.0 1 -
CHEMBL4758543 1 -
CHEMBL315108 AZUMOLENE 2.0 1 -
CHEMBL572 NITROFURANTOIN 4.0 1 -
CHEMBL4785425 1 -
CHEMBL4756680 2 -
CHEMBL1958109 THIOHYDANTOIN 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137312 DASABUVIR Ki = 4710.0 nM 5.33
CHEMBL3989927 IBERDOMIDE Ki = 4940.0 nM 5.31
CHEMBL275661 SUCCINIMIDE Ki = 8190.0 nM 5.09
CHEMBL43452 POMALIDOMIDE Ki = 10000.0 nM 5.00
CHEMBL3137312 DASABUVIR IC50 = 15600.0 nM 4.81
CHEMBL3989927 IBERDOMIDE IC50 = 16000.0 nM 4.80
CHEMBL848 LENALIDOMIDE Ki = 16300.0 nM 4.79
CHEMBL3989934 AVADOMIDE Ki = 16700.0 nM 4.78
CHEMBL275661 SUCCINIMIDE IC50 = 22300.0 nM 4.65
CHEMBL43452 POMALIDOMIDE IC50 = 25800.0 nM 4.59
CHEMBL4797970 Ki = 30800.0 nM 4.51
CHEMBL848 LENALIDOMIDE IC50 = 37800.0 nM 4.42
CHEMBL3989934 AVADOMIDE IC50 = 38700.0 nM 4.41
CHEMBL4759876 Ki = 40700.0 nM 4.39
CHEMBL4797970 IC50 = 65700.0 nM 4.18
CHEMBL4758352 Ki = 67800.0 nM 4.17
CHEMBL4759876 IC50 = 84800.0 nM 4.07
CHEMBL4756680 Ki = 229000.0 nM -
CHEMBL4785425 Activity - -
CHEMBL572 NITROFURANTOIN Activity - -
CHEMBL315108 AZUMOLENE Activity - -
CHEMBL4758543 Activity - -
CHEMBL3707254 FURAZIDIN IC50 > 1000000.0 nM -
CHEMBL100259 URIDINE Ki = 390000.0 nM -
CHEMBL1958109 THIOHYDANTOIN Ki = 169000.0 nM -
CHEMBL1958109 THIOHYDANTOIN IC50 = 332000.0 nM -
CHEMBL4758352 IC50 = 137000.0 nM -
CHEMBL30446 IC50 > 5000000.0 nM -
CHEMBL4756680 IC50 = 447000.0 nM -
CHEMBL122334 HYDANTOIN IC50 = 421000.0 nM -
CHEMBL214393 IC50 > 5000000.0 nM -
CHEMBL504 DIMETHYL SULFOXIDE Ki = 137000.0 nM -
CHEMBL504 DIMETHYL SULFOXIDE IC50 = 264000.0 nM -
CHEMBL63 ROLIPRAM IC50 = 202000.0 nM -
CHEMBL63 ROLIPRAM Ki = 102000.0 nM -
CHEMBL566 URACIL IC50 = 415000.0 nM -
CHEMBL566 URACIL Ki = 212000.0 nM -
CHEMBL1259059 SOFOSBUVIR IC50 > 1000000.0 nM -
CHEMBL100259 URIDINE IC50 = 757000.0 nM -
CHEMBL122334 HYDANTOIN Ki = 216000.0 nM -