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Assay Detail

CHEMBL4838803

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

Functional
Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay
4
Total Activities
4
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

Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.
Puxeddu M, Shen H, Bai R, Coluccia A, Bufano M, Nalli M, Sebastiani J, Brancaccio D, Da Pozzo E, Tremolanti C, Martini C, Orlando V, Biagioni S, Sinicropi MS, Ceramella J, Iacopetta D, Coluccia AML, Hamel E, Liu T, Silvestri R, La Regina G.
Eur J Med Chem (2021) 221 : 113532 -113532
PubMed 34052717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.61 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4864675 1 8.06
CHEMBL1171837 PONATINIB 4.0 1 7.97
CHEMBL4854987 1 7.88
CHEMBL1642 IMATINIB MESYLATE 4.0 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4864675 IC50 = 8.8 nM 8.06
CHEMBL1171837 PONATINIB IC50 = 10.6 nM 7.97
CHEMBL4854987 IC50 = 13.1 nM 7.88
CHEMBL1642 IMATINIB MESYLATE IC50 = 310.6 nM 6.51