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Assay Detail

CHEMBL5377329

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

Functional
Induction of apoptosis in human Imatinib-resistant K562-R3 cells incubated for 24 hrs by annexin V/PI staining based flow cytometry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Imatinib-resistant K562-R3 cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Exploiting the "Hot-Spots" of Hsp70<b>-</b>Bim Protein<b>-</b>Protein Interaction to Optimize the 1-Oxo-1<i>H</i>-phenalene-2,3-dicarbonitrile Analogues as Specific Hsp70<b>-</b>Bim Inhibitors.
Wang Z, Zhang H, Li X, Song Y, Wang Y, Hu Z, Gao Q, Jiang M, Yin F, Yuan L, Liu J, Song T, Lu S, Xu G, Zhang Z.
J Med Chem (2023) 66 : 16377 -16387
PubMed 38011535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.92 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397919 1 6.47
CHEMBL5434308 1 6.35
CHEMBL5419880 1 5.77
CHEMBL470334 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397919 EC50 = 340.0 nM 6.47
CHEMBL5434308 EC50 = 450.0 nM 6.35
CHEMBL5419880 EC50 = 1700.0 nM 5.77
CHEMBL470334 EC50 = 8500.0 nM 5.07