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Assay Detail

CHEMBL4610779

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Functional
Antiproliferative activity against human THP1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.
Zhang F, Wu Z, Chen P, Zhang J, Wang T, Zhou J, Zhang H.
Bioorg Med Chem (2020) 28 : 115228 -115228
PubMed 31813613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.77 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4640303 1 6.09
CHEMBL4647911 1 5.78
CHEMBL4636103 1 5.76
CHEMBL4633500 1 5.74
CHEMBL4637198 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4640303 IC50 = 810.0 nM 6.09
CHEMBL4647911 IC50 = 1660.0 nM 5.78
CHEMBL4636103 IC50 = 1750.0 nM 5.76
CHEMBL4633500 IC50 = 1830.0 nM 5.74
CHEMBL4637198 IC50 = 3260.0 nM 5.49