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Assay Detail

CHEMBL994209

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

Functional
Cytotoxicity against human SiHa cells after 4 hrs under strict hypoxic condition
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

SiHa (CHEMBL612542)
Type CELL-LINE
Organism Homo sapiens

Publication

Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins.
Hay MP, Hicks KO, Pchalek K, Lee HH, Blaser A, Pruijn FB, Anderson RF, Shinde SS, Wilson WR, Denny WA.
J Med Chem (2008) 51 : 6853 -6865
PubMed 18847185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.63 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451204 2 6.52
CHEMBL483193 1 6.52
CHEMBL520001 1 6.16
CHEMBL606799 1 6.16
CHEMBL606853 1 6.16
CHEMBL509303 1 6.10
CHEMBL606905 1 6.05
CHEMBL606801 1 6.00
CHEMBL606908 1 6.00
CHEMBL483374 1 5.96
CHEMBL606800 1 5.96
CHEMBL606909 1 5.92
CHEMBL443731 1 5.89
CHEMBL606854 1 5.89
CHEMBL606803 1 5.85
CHEMBL606856 1 5.80
CHEMBL520968 1 5.77
CHEMBL484379 1 5.75
CHEMBL484543 1 5.72
CHEMBL447340 1 5.62
CHEMBL50882 TIRAPAZAMINE 3.0 1 5.60
CHEMBL606907 1 5.58
CHEMBL483375 1 5.54
CHEMBL394992 1 5.54
CHEMBL483382 1 5.51
CHEMBL606906 1 5.48
CHEMBL484544 1 5.47
CHEMBL483364 1 5.47
CHEMBL484552 1 5.44
CHEMBL484214 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451204 IC50 = 300.0 nM 6.52
CHEMBL483193 IC50 = 300.0 nM 6.52
CHEMBL606799 IC50 = 700.0 nM 6.16
CHEMBL606853 IC50 = 700.0 nM 6.16
CHEMBL520001 IC50 = 700.0 nM 6.16
CHEMBL509303 IC50 = 800.0 nM 6.10
CHEMBL606905 IC50 = 900.0 nM 6.05
CHEMBL606801 IC50 = 1000.0 nM 6.00
CHEMBL606908 IC50 = 1000.0 nM 6.00
CHEMBL483374 IC50 = 1100.0 nM 5.96
CHEMBL606800 IC50 = 1100.0 nM 5.96
CHEMBL606909 IC50 = 1200.0 nM 5.92
CHEMBL443731 IC50 = 1300.0 nM 5.89
CHEMBL606854 IC50 = 1300.0 nM 5.89
CHEMBL606803 IC50 = 1400.0 nM 5.85
CHEMBL606856 IC50 = 1600.0 nM 5.80
CHEMBL520968 IC50 = 1700.0 nM 5.77
CHEMBL484379 IC50 = 1800.0 nM 5.75
CHEMBL484543 IC50 = 1900.0 nM 5.72
CHEMBL447340 IC50 = 2400.0 nM 5.62
CHEMBL50882 TIRAPAZAMINE IC50 = 2500.0 nM 5.60
CHEMBL606907 IC50 = 2600.0 nM 5.58
CHEMBL483375 IC50 = 2900.0 nM 5.54
CHEMBL394992 IC50 = 2900.0 nM 5.54
CHEMBL483382 IC50 = 3100.0 nM 5.51
CHEMBL606906 IC50 = 3300.0 nM 5.48
CHEMBL484544 IC50 = 3400.0 nM 5.47
CHEMBL483364 IC50 = 3400.0 nM 5.47
CHEMBL484552 IC50 = 3600.0 nM 5.44
CHEMBL451204 IC50 = 5000.0 nM 5.30
CHEMBL484214 IC50 = 5100.0 nM 5.29
CHEMBL483195 IC50 = 6500.0 nM 5.19
CHEMBL519490 IC50 = 8000.0 nM 5.10
CHEMBL606852 IC50 = 8400.0 nM 5.08
CHEMBL606745 IC50 = 8300.0 nM 5.08
CHEMBL606855 IC50 = 8800.0 nM 5.06
CHEMBL606802 IC50 = 13900.0 nM 4.86
CHEMBL455533 IC50 = 23000.0 nM 4.64
CHEMBL484545 IC50 = 29000.0 nM 4.54