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Assay Detail

CHEMBL5393232

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

Functional
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT4 assessed as inhibition of cell growth incubated for 96 hrs by CellTiter-Blue cell viability assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Tumor-Targeted 6-Methyl Substituted Pemetrexed and Related Antifolates with Selective Loss of RFC Transport.
Kaku K, Ravindra MP, Tong N, Choudhary S, Li X, Yu J, Karim M, Brzezinski M, O'Connor C, Hou Z, Matherly LH, Gangjee A.
ACS Med Chem Lett (2023) 14 : 1682 -1691
PubMed 38116433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.35 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433810 1 8.12
CHEMBL225072 PEMETREXED 4.0 1 7.65
CHEMBL5416929 1 7.59
CHEMBL5398059 1 7.29
CHEMBL5417031 1 7.19
CHEMBL3407519 1 7.10
CHEMBL374172 1 6.48
CHEMBL5404618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433810 IC50 = 7.66 nM 8.12
CHEMBL225072 PEMETREXED IC50 = 22.26 nM 7.65
CHEMBL5416929 IC50 = 25.9 nM 7.59
CHEMBL5398059 IC50 = 51.46 nM 7.29
CHEMBL5417031 IC50 = 64.69 nM 7.19
CHEMBL3407519 IC50 = 80.2 nM 7.10
CHEMBL374172 IC50 = 329.0 nM 6.48
CHEMBL5404618 IC50 > 1000.0 nM -