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Assay Detail

CHEMBL4398138

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

Binding
Binding affinity to human CRBN (1 to 442 residues)/N-terminal 6His-tagged human DDB1 (1 to 1140 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells after 30 mins by cy5 probe based fluorescence polarization assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BTI-TN-5B1-4
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).
Papatzimas JW, Gorobets E, Maity R, Muniyat MI, MacCallum JL, Neri P, Bahlis NJ, Derksen DJ.
J Med Chem (2019) 62 : 5522 -5540
PubMed 31117518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.72 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43452 POMALIDOMIDE 4.0 1 6.80
CHEMBL848 LENALIDOMIDE 4.0 1 6.75
CHEMBL468 THALIDOMIDE 4.0 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43452 POMALIDOMIDE Kd = 157.0 nM 6.80
CHEMBL848 LENALIDOMIDE Kd = 178.0 nM 6.75
CHEMBL468 THALIDOMIDE Kd = 250.0 nM 6.60