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Assay Detail

CHEMBL4340230

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Functional
Antiproliferative activity against human KOPTK1 cells harboring activating Notch1 gene mutations assessed as reduction in cell viability incubated for 36 hrs by MTS assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KOPTK1
Confidence 1 — Organism
Curated By Autocuration

Target

KOPTK1 (CHEMBL4483252)
Type CELL-LINE
Organism Homo sapiens

Publication

Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia.
Quaglio D, Zhdanovskaya N, Tobajas G, Cuartas V, Balducci S, Christodoulou MS, Fabrizi G, Gargantilla M, Priego EM, Carmona Pestaña Á, Passarella D, Screpanti I, Botta B, Palermo R, Mori M, Ghirga F, Pérez-Pérez MJ.
ACS Med Chem Lett (2019) 10 : 639 -643
PubMed 30996810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.75 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576806 1 6.14
CHEMBL4556946 1 5.86
CHEMBL2333805 1 5.72
CHEMBL4470333 1 5.61
CHEMBL4471467 1 5.42
CHEMBL4445762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576806 IC50 = 720.0 nM 6.14
CHEMBL4556946 IC50 = 1370.0 nM 5.86
CHEMBL2333805 IC50 = 1910.0 nM 5.72
CHEMBL4470333 IC50 = 2460.0 nM 5.61
CHEMBL4471467 IC50 = 3830.0 nM 5.42
CHEMBL4445762 IC50 - -