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Assay Detail

CHEMBL2153947

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

Functional
Antiproliferative activity against human KB cells after 48 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KB
Confidence 1 — Organism
Curated By Autocuration

Target

KB (CHEMBL398)
Type CELL-LINE
Organism Homo sapiens

Publication

Mechanism-based design, synthesis and biological studies of N⁵-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents.
Zhang Z, Tian C, Zhou S, Wang W, Guo Y, Xia J, Liu Z, Wang B, Wang X, Golding BT, Griff RJ, Du Y, Liu J.
Eur J Med Chem (2012) 58 : 228 -236
PubMed 23124219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.18 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2153710 1 6.47
CHEMBL2153707 1 5.57
CHEMBL2153703 1 5.17
CHEMBL2153712 1 4.70
CHEMBL34259 METHOTREXATE 4.0 1 4.68
CHEMBL2151066 1 4.51
CHEMBL2153705 1 -
CHEMBL2153704 1 -
CHEMBL2153706 1 -
CHEMBL2153708 1 -
CHEMBL2153711 1 -
CHEMBL2153713 1 -
CHEMBL2153714 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2153710 IC50 = 336.0 nM 6.47
CHEMBL2153707 IC50 = 2700.0 nM 5.57
CHEMBL2153703 IC50 = 6722.0 nM 5.17
CHEMBL2153712 IC50 = 20030.0 nM 4.70
CHEMBL34259 METHOTREXATE IC50 = 20900.0 nM 4.68
CHEMBL2151066 IC50 = 31050.0 nM 4.51
CHEMBL2153705 IC50 > 100000.0 nM -
CHEMBL2153704 IC50 > 100000.0 nM -
CHEMBL2153706 IC50 > 100000.0 nM -
CHEMBL2153708 IC50 > 100000.0 nM -
CHEMBL2153711 IC50 > 130000.0 nM -
CHEMBL2153713 IC50 > 100000.0 nM -
CHEMBL2153714 IC50 > 100000.0 nM -