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Assay Detail

CHEMBL1003011

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Functional
Antiproliferative activity against chinese hamster RT16 cells expressing human folate receptor alpha after 96 hrs by celltiter-blue cell viability assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Cell Type RT16
Confidence 1 — Organism
Curated By Autocuration

Publication

Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry.
Deng Y, Zhou X, Kugel Desmoulin S, Wu J, Cherian C, Hou Z, Matherly LH, Gangjee A.
J Med Chem (2009) 52 : 2940 -2951
PubMed 19371039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.54 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491104 1 8.05
CHEMBL490934 1 7.89
CHEMBL491129 1 7.25
CHEMBL491298 1 6.97
CHEMBL522455 1 -
CHEMBL522126 1 -
CHEMBL491299 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491104 IC50 = 9.0 nM 8.05
CHEMBL490934 IC50 = 13.0 nM 7.89
CHEMBL491129 IC50 = 56.0 nM 7.25
CHEMBL491298 IC50 = 108.0 nM 6.97
CHEMBL522455 IC50 > 1000.0 nM -
CHEMBL522126 IC50 > 1000.0 nM -
CHEMBL491299 IC50 > 1000.0 nM -