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Assay Detail

CHEMBL5133516

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Functional
Antiproliferative activity against human A-431 cells overexpressing EGFR assessed as cell growth inhibition 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 A-431
Confidence 1 — Organism
Curated By Autocuration

Target

A-431 (CHEMBL614069)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of potent antiproliferative agents from selected oxygen heterocycles as EGFR tyrosine kinase inhibitors from the U.S. National Cancer Institute database by in silico screening and bioactivity evaluation.
Jiwacharoenchai N, Saruengkhanphasit R, Niwetmarin W, Seetaha S, Choowongkomon K, Ruchirawat S, Eurtivong C.
Bioorg Med Chem Lett (2022) 58 : 128524 -128524
PubMed 34995690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.10 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478960 MACLURAXANTHONE 1 5.55
CHEMBL5192793 1 5.42
CHEMBL5181037 1 5.22
CHEMBL323197 MANGOSTIN 1 5.14
CHEMBL5185036 1 4.75
CHEMBL553 ERLOTINIB 4.0 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478960 MACLURAXANTHONE IC50 = 2840.0 nM 5.55
CHEMBL5192793 IC50 = 3810.0 nM 5.42
CHEMBL5181037 IC50 = 6040.0 nM 5.22
CHEMBL323197 MANGOSTIN IC50 = 7200.0 nM 5.14
CHEMBL5185036 IC50 = 17710.0 nM 4.75
CHEMBL553 ERLOTINIB IC50 = 31940.0 nM 4.50