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Assay Detail

CHEMBL2051659

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

Functional
Cytotoxicity against human HT-29 cells after 48 hrs by XTT assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Autocuration

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents.
Yamazaki Y, Sumikura M, Masuda Y, Hayashi Y, Yasui H, Kiso Y, Chinen T, Usui T, Yakushiji F, Potts B, Neuteboom S, Palladino M, Lloyd GK, Hayashi Y.
Bioorg Med Chem (2012) 20 : 4279 -4289
PubMed 22727370 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.46 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2048720 1 9.30
CHEMBL2048719 1 9.22
CHEMBL2048723 1 8.96
CHEMBL2048722 1 8.70
CHEMBL2048718 1 8.52
CHEMBL2048713 1 8.42
CHEMBL2048724 1 8.40
CHEMBL2048721 1 8.22
CHEMBL107 COLCHICINE 4.0 1 8.03
CHEMBL2048712 1 7.41
CHEMBL2048709 1 7.39
CHEMBL2048725 1 6.83
CHEMBL2048711 1 6.44
CHEMBL2048714 1 6.02
CHEMBL2048708 1 5.92
CHEMBL2048715 1 5.75
CHEMBL2048717 1 5.60
CHEMBL2048716 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2048720 IC50 = 0.5 nM 9.30
CHEMBL2048719 IC50 = 0.6 nM 9.22
CHEMBL2048723 IC50 = 1.1 nM 8.96
CHEMBL2048722 IC50 = 2.0 nM 8.70
CHEMBL2048718 IC50 = 3.0 nM 8.52
CHEMBL2048713 IC50 = 3.8 nM 8.42
CHEMBL2048724 IC50 = 4.0 nM 8.40
CHEMBL2048721 IC50 = 6.0 nM 8.22
CHEMBL107 COLCHICINE IC50 = 9.3 nM 8.03
CHEMBL2048712 IC50 = 39.0 nM 7.41
CHEMBL2048709 IC50 = 41.0 nM 7.39
CHEMBL2048725 IC50 = 147.0 nM 6.83
CHEMBL2048711 IC50 = 360.0 nM 6.44
CHEMBL2048714 IC50 = 955.0 nM 6.02
CHEMBL2048708 IC50 = 1200.0 nM 5.92
CHEMBL2048715 IC50 = 1800.0 nM 5.75
CHEMBL2048717 IC50 = 2500.0 nM 5.60
CHEMBL2048716 IC50 = 7300.0 nM 5.14