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Assay Detail

CHEMBL5242499

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

Functional
Cytotoxicity against human NCI-H358 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H358
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H358 (CHEMBL614135)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology.
Heinrich T, Sala-Hojman A, Ferretti R, Petersson C, Minguzzi S, Gondela A, Ramaswamy S, Bartosik A, Czauderna F, Crowley L, Wahra P, Schilke H, Böpple P, Dudek Ł, Leś M, Niedziejko P, Olech K, Pawlik H, Włoszczak Ł, Zuchowicz K, Suarez Alvarez JR, Martyka J, Sitek E, Mikulski M, Szczęśniak J, Jäckel S, Krier M, Król M, Wegener A, Gałęzowski M, Nowak M, Becker F, Herhaus C.
J Med Chem (2021) 64 : 11904 -11933
PubMed 34382802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4802043 MSC-4381 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4802043 MSC-4381 IC50 = 3.0 nM 8.52