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Assay Detail

CHEMBL2025198

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

Functional
Cytotoxicity against human HCT116 cells after 48 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
Type CELL-LINE
Organism Homo sapiens

Publication

Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
Chen QY, Liu Y, Luesch H.
ACS Med Chem Lett (2011) 2 : 861 -865
PubMed 22081789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.58 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022564 APRATOXIN S4 1 8.94
CHEMBL2022566 APRATOXIN S6 1 8.80
CHEMBL2022562 APRATOXIN S2 1 8.38
CHEMBL2022560 APRATOXIN F 1 8.31
CHEMBL501696 APRATOXIN A 1 8.22
CHEMBL506311 APRATOXIN E 1 6.74
CHEMBL2022565 APRATOXIN S5 1 6.59
CHEMBL2022561 APRATOXIN S1 1 6.43
CHEMBL2022563 APRATOXIN S3 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022564 APRATOXIN S4 IC50 = 1.14 nM 8.94
CHEMBL2022566 APRATOXIN S6 IC50 = 1.58 nM 8.80
CHEMBL2022562 APRATOXIN S2 IC50 = 4.13 nM 8.38
CHEMBL2022560 APRATOXIN F IC50 = 4.92 nM 8.31
CHEMBL501696 APRATOXIN A IC50 = 5.97 nM 8.22
CHEMBL506311 APRATOXIN E IC50 = 184.0 nM 6.74
CHEMBL2022565 APRATOXIN S5 IC50 = 258.0 nM 6.59
CHEMBL2022561 APRATOXIN S1 IC50 = 373.0 nM 6.43
CHEMBL2022563 APRATOXIN S3 IC50 = 1700.0 nM 5.77