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Assay Detail

CHEMBL693199

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

Functional
Ability of compound to inhibit [3H]MTX influx in Hela cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Intermediate

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
Nair MG, Bridges TW, Henkel TJ, Kisliuk RL, Gaumont Y, Sirotnak FM.
J Med Chem (1981) 24 : 1068 -1073
PubMed 6793726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.21 6.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10804 1 6.13
CHEMBL10591 1 5.57
CHEMBL11133 ISOAMINOPTERIN 1 5.05
CHEMBL11187 1 4.68
CHEMBL10592 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10804 IC50 = 740.0 nM 6.13
CHEMBL10591 IC50 = 2700.0 nM 5.57
CHEMBL11133 ISOAMINOPTERIN IC50 = 9000.0 nM 5.05
CHEMBL11187 IC50 = 21000.0 nM 4.68
CHEMBL10592 IC50 = 25000.0 nM 4.60