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Assay Detail

CHEMBL4268530

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

Functional
Cytotoxicity against human HepG2A16 cells expressing GFP-fused CD81 after 48 hrs by bioluminescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.
Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T, Avery VM, Winzeler EA, Held J, Andrews KT, Hansen FK.
Eur J Med Chem (2018) 158 : 801 -813
PubMed 30245402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.96 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 5.60
CHEMBL4162282 1 5.24
CHEMBL4278449 1 5.16
CHEMBL4063658 1 5.11
CHEMBL4292530 1 5.00
CHEMBL4288073 1 4.92
CHEMBL4281918 1 4.91
CHEMBL4276668 1 4.67
CHEMBL4173361 1 4.67
CHEMBL4283545 1 4.66
CHEMBL4289151 1 4.59
CHEMBL1450 ATOVAQUONE 4.0 1 -
CHEMBL4280840 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 2510.0 nM 5.60
CHEMBL4162282 IC50 = 5810.0 nM 5.24
CHEMBL4278449 IC50 = 6990.0 nM 5.16
CHEMBL4063658 IC50 = 7800.0 nM 5.11
CHEMBL4292530 IC50 = 9990.0 nM 5.00
CHEMBL4288073 IC50 = 11900.0 nM 4.92
CHEMBL4281918 IC50 = 12340.0 nM 4.91
CHEMBL4276668 IC50 = 21390.0 nM 4.67
CHEMBL4173361 IC50 = 21150.0 nM 4.67
CHEMBL4283545 IC50 = 21980.0 nM 4.66
CHEMBL4289151 IC50 = 25940.0 nM 4.59
CHEMBL1450 ATOVAQUONE IC50 > 500.0 nM -
CHEMBL4280840 IC50 > 50000.0 nM -