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Assay Detail

CHEMBL5537733

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

Functional
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
16
Total Activities
16
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

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 16 6.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 9.00
CHEMBL325041 BORTEZOMIB 3.0 1 8.20
CHEMBL98 VORINOSTAT 4.0 1 6.75
CHEMBL3692688 1 5.03
CHEMBL3110004 1 4.89
CHEMBL5579748 1 4.33
CHEMBL5563683 1 -
CHEMBL5571522 1 -
CHEMBL5570082 1 -
CHEMBL5572569 1 -
CHEMBL5571764 1 -
CHEMBL5571685 1 -
CHEMBL3692573 1 -
CHEMBL5572470 1 -
CHEMBL5571546 1 -
CHEMBL5575926 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 1.0 nM 9.00
CHEMBL325041 BORTEZOMIB IC50 = 6.28 nM 8.20
CHEMBL98 VORINOSTAT IC50 = 180.0 nM 6.75
CHEMBL3692688 IC50 = 9240.0 nM 5.03
CHEMBL3110004 IC50 = 13000.0 nM 4.89
CHEMBL5579748 IC50 = 47300.0 nM 4.33
CHEMBL5563683 IC50 > 100000.0 nM -
CHEMBL5571522 IC50 ~ 100000.0 nM -
CHEMBL5570082 IC50 > 100000.0 nM -
CHEMBL5572569 IC50 ~ 100000.0 nM -
CHEMBL5571764 IC50 > 100000.0 nM -
CHEMBL5571685 IC50 ~ 100000.0 nM -
CHEMBL3692573 IC50 > 100000.0 nM -
CHEMBL5572470 IC50 ~ 100000.0 nM -
CHEMBL5571546 IC50 ~ 100000.0 nM -
CHEMBL5575926 IC50 ~ 100000.0 nM -