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Assay Detail

CHEMBL4768022

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Functional
Antiproliferative activity against human H1299 cells assessed as reduction in cell viability by MTS assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1299
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1299 (CHEMBL612255)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis and biological activity of N-substituted tetrahydropteroate analogs as non-classical antifolates against cobalamin-dependent methionine synthase and potential anticancer agents.
Wang M,Tian C,Xue L,Li H,Cong J,Fang F,Yang J,Yuan M,Chen Y,Guo Y,Wang X,Liu J,Zhang Z
Eur J Med Chem (2020) 190 : 112113 -112113
PubMed 32058237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.03 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4776344 1 7.31
CHEMBL34259 METHOTREXATE 4.0 1 7.14
CHEMBL4777807 1 7.03
CHEMBL4796741 1 6.92
CHEMBL4778495 1 6.80
CHEMBL4787377 1 6.68
CHEMBL4789573 1 6.64
CHEMBL4798756 1 6.62
CHEMBL4794524 1 6.39
CHEMBL4798785 1 6.36
CHEMBL4788657 1 6.33
CHEMBL4794744 1 6.24
CHEMBL4791051 1 6.18
CHEMBL4795611 1 6.00
CHEMBL4793123 1 5.01
CHEMBL4782321 1 4.80
CHEMBL4794394 1 4.75
CHEMBL4781661 1 4.73
CHEMBL4793044 1 4.50
CHEMBL4799637 1 4.07
CHEMBL4792336 1 -
CHEMBL4786618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4776344 IC50 = 49.0 nM 7.31
CHEMBL34259 METHOTREXATE IC50 = 72.0 nM 7.14
CHEMBL4777807 IC50 = 93.0 nM 7.03
CHEMBL4796741 IC50 = 120.0 nM 6.92
CHEMBL4778495 IC50 = 160.0 nM 6.80
CHEMBL4787377 IC50 = 210.0 nM 6.68
CHEMBL4789573 IC50 = 230.0 nM 6.64
CHEMBL4798756 IC50 = 240.0 nM 6.62
CHEMBL4794524 IC50 = 410.0 nM 6.39
CHEMBL4798785 IC50 = 440.0 nM 6.36
CHEMBL4788657 IC50 = 470.0 nM 6.33
CHEMBL4794744 IC50 = 570.0 nM 6.24
CHEMBL4791051 IC50 = 660.0 nM 6.18
CHEMBL4795611 IC50 = 990.0 nM 6.00
CHEMBL4793123 IC50 = 9750.0 nM 5.01
CHEMBL4782321 IC50 = 15900.0 nM 4.80
CHEMBL4794394 IC50 = 17700.0 nM 4.75
CHEMBL4781661 IC50 = 18500.0 nM 4.73
CHEMBL4793044 IC50 = 32000.0 nM 4.50
CHEMBL4799637 IC50 = 85300.0 nM 4.07
CHEMBL4792336 IC50 > 100000.0 nM -
CHEMBL4786618 IC50 > 100000.0 nM -