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Assay Detail

CHEMBL4274356

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Functional
Antiproliferative activity against human HeLa cells after 72 hrs by Coulter counter method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HeLa
Confidence 1 — Organism
Curated By Intermediate

Target

HeLa (CHEMBL399)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis of a 3'-C-ethynyl-β-d-ribofuranose purine nucleoside library: Discovery of C7-deazapurine analogs as potent antiproliferative nucleosides.
Hulpia F, Noppen S, Schols D, Andrei G, Snoeck R, Liekens S, Vervaeke P, Van Calenbergh S.
Eur J Med Chem (2018) 157 : 248 -267
PubMed 30098481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.18 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4276891 1 7.29
CHEMBL4287532 1 7.03
CHEMBL4277322 1 6.82
CHEMBL4295176 1 6.75
CHEMBL4281756 1 6.75
CHEMBL2094094 1 6.54
CHEMBL4281102 1 6.12
CHEMBL4284518 1 6.06
CHEMBL4281512 1 6.05
CHEMBL4289398 1 5.96
CHEMBL4288972 1 5.77
CHEMBL4284939 1 5.36
CHEMBL4292803 1 5.20
CHEMBL4291736 1 4.85
CHEMBL4288324 1 -
CHEMBL4277684 1 -
CHEMBL4278293 1 -
CHEMBL4285278 1 -
CHEMBL4280712 1 -
CHEMBL4288621 1 -
CHEMBL4289054 1 -
CHEMBL4278380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4276891 IC50 = 51.0 nM 7.29
CHEMBL4287532 IC50 = 93.0 nM 7.03
CHEMBL4277322 IC50 = 150.0 nM 6.82
CHEMBL4295176 IC50 = 180.0 nM 6.75
CHEMBL4281756 IC50 = 180.0 nM 6.75
CHEMBL2094094 IC50 = 290.0 nM 6.54
CHEMBL4281102 IC50 = 750.0 nM 6.12
CHEMBL4284518 IC50 = 880.0 nM 6.06
CHEMBL4281512 IC50 = 890.0 nM 6.05
CHEMBL4289398 IC50 = 1100.0 nM 5.96
CHEMBL4288972 IC50 = 1700.0 nM 5.77
CHEMBL4284939 IC50 = 4400.0 nM 5.36
CHEMBL4292803 IC50 = 6300.0 nM 5.20
CHEMBL4291736 IC50 = 14000.0 nM 4.85
CHEMBL4288324 IC50 > 250000.0 nM -
CHEMBL4277684 IC50 = 114000.0 nM -
CHEMBL4278293 IC50 = 135000.0 nM -
CHEMBL4285278 IC50 = 220000.0 nM -
CHEMBL4280712 IC50 = 170000.0 nM -
CHEMBL4288621 IC50 > 250000.0 nM -
CHEMBL4289054 IC50 > 250000.0 nM -
CHEMBL4278380 IC50 > 250000.0 nM -