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Assay Detail

CHEMBL2016076

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

Functional
Cytotoxicity against human K562 cells after 72 hrs by MTS assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type K562
Confidence 1 — Organism
Curated By Autocuration

Target

K562 (CHEMBL385)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel bifendate derivatives bearing 6,7-dihydro-dibenzo[c,e]azepine scaffold as potent P-glycoprotein inhibitors.
Gu X, Ren Z, Tang X, Peng H, Zhao Q, Lai Y, Peng S, Zhang Y.
Eur J Med Chem (2012) 51 : 137 -144
PubMed 22405646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.64 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 6.37
CHEMBL2012366 1 4.38
CHEMBL2012368 1 4.36
CHEMBL2012362 1 4.34
CHEMBL2012363 1 4.27
CHEMBL2012356 1 4.11
CHEMBL2012355 1 -
CHEMBL2012357 1 -
CHEMBL2012358 1 -
CHEMBL2012359 1 -
CHEMBL2012360 1 -
CHEMBL2012361 1 -
CHEMBL2012364 1 -
CHEMBL2012365 1 -
CHEMBL2012367 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 430.0 nM 6.37
CHEMBL2012366 IC50 = 41710.0 nM 4.38
CHEMBL2012368 IC50 = 43480.0 nM 4.36
CHEMBL2012362 IC50 = 45360.0 nM 4.34
CHEMBL2012363 IC50 = 53720.0 nM 4.27
CHEMBL2012356 IC50 = 77470.0 nM 4.11
CHEMBL2012355 IC50 = 125000.0 nM -
CHEMBL2012357 IC50 > 100000.0 nM -
CHEMBL2012358 IC50 > 200000.0 nM -
CHEMBL2012359 IC50 = 106000.0 nM -
CHEMBL2012360 IC50 > 100000.0 nM -
CHEMBL2012361 IC50 = 140300.0 nM -
CHEMBL2012364 IC50 > 200000.0 nM -
CHEMBL2012365 IC50 > 100000.0 nM -
CHEMBL2012367 IC50 > 100000.0 nM -