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Assay Detail

CHEMBL4624218

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

Binding
Inhibition of DHFR in Chinese Hamster MTXRII-OuaR2-4 R2 cells expressing human PCFT assessed as reduction in cell growth after 96 hrs by Cell-Titer Blue assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cricetulus griseus
Cell Type R2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.
Golani LK, Islam F, O'Connor C, Dekhne AS, Hou Z, Matherly LH, Gangjee A.
Bioorg Med Chem (2020) 28 : 115544 -115544
PubMed 32503687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.40 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225072 PEMETREXED 4.0 1 7.88
CHEMBL34259 METHOTREXATE 4.0 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225072 PEMETREXED IC50 = 13.2 nM 7.88
CHEMBL34259 METHOTREXATE IC50 = 121.0 nM 6.92