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Assay Detail

CHEMBL4194628

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

ADMET
Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.
Ravindra M, Wallace-Povirk A, Karim MA, Wilson MR, O'Connor C, White K, Kushner J, Polin L, George C, Hou Z, Matherly LH, Gangjee A.
J Med Chem (2018) 61 : 2027 -2040
PubMed 29425443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.73 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225071 RALTITREXED 4.0 1 7.82
CHEMBL34259 METHOTREXATE 4.0 1 6.94
CHEMBL1201746 PRALATREXATE 4.0 1 6.09
CHEMBL225072 PEMETREXED 4.0 1 6.07
CHEMBL365307 1 -
CHEMBL4205344 1 -
CHEMBL4214638 1 -
CHEMBL4209721 1 -
CHEMBL4218109 1 -
CHEMBL4213181 1 -
CHEMBL4205885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225071 RALTITREXED IC50 = 15.0 nM 7.82
CHEMBL34259 METHOTREXATE IC50 = 114.0 nM 6.94
CHEMBL1201746 PRALATREXATE IC50 = 819.0 nM 6.09
CHEMBL225072 PEMETREXED IC50 = 849.0 nM 6.07
CHEMBL365307 IC50 > 1000.0 nM -
CHEMBL4205344 IC50 > 1000.0 nM -
CHEMBL4214638 IC50 > 1000.0 nM -
CHEMBL4209721 IC50 > 1000.0 nM -
CHEMBL4218109 IC50 > 1000.0 nM -
CHEMBL4213181 IC50 > 1000.0 nM -
CHEMBL4205885 IC50 > 1000.0 nM -