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Assay Detail

CHEMBL4316283

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

Functional
Cytotoxicity against human KBM5 cells expressing IM-resistant Bcr/Abl T315I mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KBM5
Confidence 1 — Organism
Curated By Autocuration

Target

KBM5 (CHEMBL4483250)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies.
Puxeddu M, Shen H, Bai R, Coluccia A, Nalli M, Mazzoccoli C, Da Pozzo E, Cavallini C, Martini C, Orlando V, Biagioni S, Mazzoni C, Coluccia AML, Hamel E, Liu T, Silvestri R, La Regina G.
Eur J Med Chem (2020) 185 : 111828 -111828
PubMed 31727471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.38 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4536640 1 7.92
CHEMBL4559506 1 7.80
CHEMBL4543075 1 7.68
CHEMBL4444616 1 7.66
CHEMBL4586068 1 7.58
CHEMBL255863 NILOTINIB 4.0 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4536640 IC50 = 12.0 nM 7.92
CHEMBL4559506 IC50 = 16.0 nM 7.80
CHEMBL4543075 IC50 = 21.0 nM 7.68
CHEMBL4444616 IC50 = 22.0 nM 7.66
CHEMBL4586068 IC50 = 26.0 nM 7.58
CHEMBL255863 NILOTINIB IC50 = 2421.0 nM 5.62