Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3632250

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

Binding
Binding affinity to human RFC expressed in Chinese hamster PC43-10 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC43-10
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Reduced folate transporter (CHEMBL4833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.
Wang L, Wallace A, Raghavan S, Deis SM, Wilson MR, Yang S, Polin L, White K, Kushner J, Orr S, George C, O'Connor C, Hou Z, Mitchell-Ryan S, Dann CE, Matherly LH, Gangjee A.
J Med Chem (2015) 58 : 6938 -6959
PubMed 26317331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.93 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3628345 1 7.27
CHEMBL1834488 1 7.00
CHEMBL3628346 1 6.72
CHEMBL3628344 1 6.71
CHEMBL3628347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3628345 IC50 = 54.0 nM 7.27
CHEMBL1834488 IC50 = 101.0 nM 7.00
CHEMBL3628346 IC50 = 189.0 nM 6.72
CHEMBL3628344 IC50 = 197.0 nM 6.71
CHEMBL3628347 IC50 > 1000.0 nM -