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Assay Detail

CHEMBL656266

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

Functional
In vitro cytotoxicity by its growth inhibitory activity against human leukemic lymphoblasts (CEM cells).
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CCRF-CEM
Confidence 1 — Organism
Curated By Intermediate

Target

CCRF-CEM (CHEMBL382)
Type CELL-LINE
Organism Homo sapiens

Publication

Methotrexate analogues. 21. Divergent influence of alkyl chain length on the dihydrofolate reductase affinity and cytotoxicity of methotrexate monoesters.
Rosowsky A, Forsch RA, Yu CS, Lazarus H, Beardsley GP.
J Med Chem (1984) 27 : 605 -609
PubMed 6585550 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.37 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34259 METHOTREXATE 4.0 1 7.60
CHEMBL351766 1 6.96
CHEMBL157083 1 6.60
CHEMBL351765 1 6.43
CHEMBL155016 1 6.11
CHEMBL154152 1 6.04
CHEMBL157904 1 5.70
CHEMBL347439 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34259 METHOTREXATE IC50 = 25.0 nM 7.60
CHEMBL351766 IC50 = 110.0 nM 6.96
CHEMBL157083 IC50 = 250.0 nM 6.60
CHEMBL351765 IC50 = 370.0 nM 6.43
CHEMBL155016 IC50 = 780.0 nM 6.11
CHEMBL154152 IC50 = 920.0 nM 6.04
CHEMBL157904 IC50 = 2000.0 nM 5.70
CHEMBL347439 IC50 = 3000.0 nM 5.52