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Assay Detail

CHEMBL5537765

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Functional
Antiproliferative activity against human CAL-27 cells overexpressing HDAC4 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CAL-27
Confidence 1 — Organism
Curated By Autocuration

Target

CAL-27 (CHEMBL1075408)
Type CELL-LINE
Organism Homo sapiens

Publication

5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib.
Asfaha Y, Bollmann LM, Skerhut AJ, Fischer F, Horstick N, Roth D, Wecker M, Mammen C, Smits SHJ, Fluegen G, Kassack MU, Kurz T.
Eur J Med Chem (2024) 263 : 115907 -115907
PubMed 37979441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.86 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325041 BORTEZOMIB 3.0 1 5.33
CHEMBL3692688 1 5.06
CHEMBL4456445 1 4.89
CHEMBL5571546 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325041 BORTEZOMIB IC50 = 4730.0 nM 5.33
CHEMBL3692688 IC50 = 8630.0 nM 5.06
CHEMBL4456445 IC50 = 12800.0 nM 4.89
CHEMBL5571546 IC50 = 69800.0 nM 4.16