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Assay Detail

CHEMBL5385190

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

Functional
Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK-8 assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 1 — Organism
Curated By Autocuration

Target

A549 (CHEMBL392)
Type CELL-LINE
Organism Homo sapiens

Publication

Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
Qiu Q, Chi F, Zhou D, Xie Z, Liu Y, Wu H, Yin Z, Shi W, Qian H.
J Med Chem (2023) 66 : 5753 -5773
PubMed 37057760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.73 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433552 1 6.14
CHEMBL5395502 1 5.90
CHEMBL5432341 1 5.84
CHEMBL5437969 1 5.83
CHEMBL1287853 FEDRATINIB 4.0 1 5.76
CHEMBL98 VORINOSTAT 4.0 1 5.75
CHEMBL5440597 1 5.69
CHEMBL5409823 1 5.67
CHEMBL5424724 1 5.65
CHEMBL5427399 1 5.63
CHEMBL5418300 1 5.54
CHEMBL5403924 1 5.53
CHEMBL5427372 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433552 IC50 = 730.0 nM 6.14
CHEMBL5395502 IC50 = 1270.0 nM 5.90
CHEMBL5432341 IC50 = 1430.0 nM 5.84
CHEMBL5437969 IC50 = 1490.0 nM 5.83
CHEMBL1287853 FEDRATINIB IC50 = 1730.0 nM 5.76
CHEMBL98 VORINOSTAT IC50 = 1790.0 nM 5.75
CHEMBL5440597 IC50 = 2030.0 nM 5.69
CHEMBL5409823 IC50 = 2160.0 nM 5.67
CHEMBL5424724 IC50 = 2240.0 nM 5.65
CHEMBL5427399 IC50 = 2330.0 nM 5.63
CHEMBL5418300 IC50 = 2910.0 nM 5.54
CHEMBL5403924 IC50 = 2950.0 nM 5.53
CHEMBL5427372 IC50 = 3080.0 nM 5.51