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Assay Detail

CHEMBL5519642

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

Functional
Antiproliferative activity against human U-937 cells incubated for 72 hrs
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Autocuration

Target

U-937 (CHEMBL612794)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of the cereblon-recruiting tubulin PROTACs effective in overcoming Taxol resistance in vitro and in vivo.
Yang H, Qin J, Pei Y, Guan S, Zhao M, Wang Y, Yao Y, Duan Y, Sun M.
Eur J Med Chem (2024) 265 : 116067 -116067
PubMed 38171146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.94 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL67 COMBRETASTATIN A4 -1.0 1 9.52
CHEMBL5562001 1 8.22
CHEMBL5559529 1 7.75
CHEMBL5560424 1 7.66
CHEMBL5563800 1 6.10
CHEMBL5563040 1 5.79
CHEMBL5565213 1 5.37
CHEMBL5549800 1 5.07
CHEMBL5559137 1 -
CHEMBL5559483 1 -
CHEMBL5542417 1 -
CHEMBL5555894 1 -
CHEMBL5568500 1 -
CHEMBL5566922 1 -
CHEMBL5542736 1 -
CHEMBL5556632 1 -
CHEMBL5559164 1 -
CHEMBL5560260 1 -
CHEMBL5556498 1 -
CHEMBL5560499 1 -
CHEMBL5542218 1 -
CHEMBL5542200 1 -
CHEMBL5557986 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL67 COMBRETASTATIN A4 IC50 = 0.3 nM 9.52
CHEMBL5562001 IC50 = 6.0 nM 8.22
CHEMBL5559529 IC50 = 18.0 nM 7.75
CHEMBL5560424 IC50 = 22.0 nM 7.66
CHEMBL5563800 IC50 = 800.0 nM 6.10
CHEMBL5563040 IC50 = 1622.0 nM 5.79
CHEMBL5565213 IC50 = 4316.0 nM 5.37
CHEMBL5549800 IC50 = 8594.0 nM 5.07
CHEMBL5559137 IC50 > 5000.0 nM -
CHEMBL5559483 IC50 > 5000.0 nM -
CHEMBL5542417 IC50 > 5000.0 nM -
CHEMBL5555894 IC50 > 5000.0 nM -
CHEMBL5568500 IC50 > 5000.0 nM -
CHEMBL5566922 IC50 > 5000.0 nM -
CHEMBL5542736 IC50 > 5000.0 nM -
CHEMBL5556632 IC50 > 5000.0 nM -
CHEMBL5559164 IC50 > 5000.0 nM -
CHEMBL5560260 IC50 > 5000.0 nM -
CHEMBL5556498 IC50 > 5000.0 nM -
CHEMBL5560499 IC50 > 5000.0 nM -
CHEMBL5542218 IC50 > 5000.0 nM -
CHEMBL5542200 IC50 > 5000.0 nM -
CHEMBL5557986 IC50 > 5000.0 nM -