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Assay Detail

CHEMBL1067628

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Functional
Growth inhibition of Chinese hamster RT16 cells expressing human FRalpha in presence of 200 nM folic acid after 96 hrs
4
Total Activities
4
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 antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
Wang L, Cherian C, Desmoulin SK, Polin L, Deng Y, Wu J, Hou Z, White K, Kushner J, Matherly LH, Gangjee A.
J Med Chem (2010) 53 : 1306 -1318
PubMed 20085328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.06 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL590985 TALOTREXIN 2.0 1 6.06
CHEMBL590740 1 -
CHEMBL605580 1 -
CHEMBL601009 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL590985 TALOTREXIN IC50 = 864.0 nM 6.06
CHEMBL590740 IC50 > 1000.0 nM -
CHEMBL605580 IC50 > 1000.0 nM -
CHEMBL601009 IC50 > 1000.0 nM -