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Assay Detail

CHEMBL5505657

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

Functional
Induction of radiosensitization against human HCT116/54C cells assessed as potentiation of radiation-induced cytotoxicity pre-irradiated with gamma radiation at 3 Gy followed by incubation with drug for 1 hr and measured after 18 hrs by SRB method normalized to radiation only
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT116/54C
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of 6-Anilino Imidazo[4,5-<i>c</i>]pyridin-2-ones as Selective DNA-Dependent Protein Kinase Inhibitors and Their Application as Radiosensitizers.
Hong CR, Liew LP, Wong WW, Dickson BD, Cheng G, Shome A, Airey R, Jaiswal J, Lipert B, Jamieson SMF, Wilson WR, Hay MP.
J Med Chem (2024) 67 : 12366 -12385
PubMed 39007759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.14 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439259 AZD-7648 1.0 1 7.21
CHEMBL5527881 1 6.68
CHEMBL5532026 1 6.68
CHEMBL5558866 1 6.66
CHEMBL4297629 NEDISERTIB 1.0 1 6.58
CHEMBL5531947 1 6.51
CHEMBL5559388 1 6.43
CHEMBL5556014 1 6.40
CHEMBL5517961 1 6.40
CHEMBL5542350 1 6.27
CHEMBL5542587 1 6.08
CHEMBL5559345 1 6.05
CHEMBL5559285 1 6.03
CHEMBL5558337 1 5.86
CHEMBL5523360 1 5.84
CHEMBL5517925 1 5.77
CHEMBL5523472 1 5.68
CHEMBL5543038 1 5.32
CHEMBL5542141 1 5.20
CHEMBL5532012 1 5.13
CHEMBL5532346 1 -
CHEMBL5555156 1 -
CHEMBL6067692 1 -
CHEMBL5558970 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439259 AZD-7648 IC50 = 61.0 nM 7.21
CHEMBL5527881 IC50 = 210.0 nM 6.68
CHEMBL5532026 IC50 = 210.0 nM 6.68
CHEMBL5558866 IC50 = 220.0 nM 6.66
CHEMBL4297629 NEDISERTIB IC50 = 260.0 nM 6.58
CHEMBL5531947 IC50 = 310.0 nM 6.51
CHEMBL5559388 IC50 = 370.0 nM 6.43
CHEMBL5556014 IC50 = 400.0 nM 6.40
CHEMBL5517961 IC50 = 400.0 nM 6.40
CHEMBL5542350 IC50 = 540.0 nM 6.27
CHEMBL5542587 IC50 = 830.0 nM 6.08
CHEMBL5559345 IC50 = 890.0 nM 6.05
CHEMBL5559285 IC50 = 930.0 nM 6.03
CHEMBL5558337 IC50 = 1380.0 nM 5.86
CHEMBL5523360 IC50 = 1460.0 nM 5.84
CHEMBL5517925 IC50 = 1710.0 nM 5.77
CHEMBL5523472 IC50 = 2100.0 nM 5.68
CHEMBL5543038 IC50 = 4760.0 nM 5.32
CHEMBL5542141 IC50 = 6300.0 nM 5.20
CHEMBL5532012 IC50 = 7410.0 nM 5.13
CHEMBL5532346 IC50 - -
CHEMBL5555156 IC50 - -
CHEMBL6067692 IC50 > 10000.0 nM -
CHEMBL5558970 IC50 > 10000.0 nM -