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Assay Detail

CHEMBL3705063

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Binding
Cellular Assay: ATM and ATR have distinct and overlapping responses to DNA damage. They must participate together and responses must be co-ordinated. Both pathways may be activated by ionising radiation, however only ATR is activated by UV. Since UV treatment is not practical for use in a high throught-put cell assay, the UV mimetic 4NQ0 (Sigma) was chosen to activate the ATR DNA damage response pathway.
27
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase ATR (CHEMBL5024)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chemical compounds
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.52 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3648331 2 8.59
CHEMBL3648329 1 8.15
CHEMBL3648334 2 8.07
CHEMBL3648341 2 8.00
CHEMBL3648330 2 7.89
CHEMBL3648333 1 7.86
CHEMBL3648340 2 7.79
CHEMBL3648328 2 7.66
CHEMBL3648339 2 7.54
CHEMBL3648338 2 7.48
CHEMBL3648335 2 7.40
CHEMBL3648336 1 7.29
CHEMBL4285417 CERALASERTIB 3.0 1 7.23
CHEMBL3648337 2 7.20
CHEMBL3648332 2 6.96
CHEMBL3648327 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3648331 IC50 = 2.578 nM 8.59
CHEMBL3648331 IC50 = 2.757 nM 8.56
CHEMBL3648329 IC50 = 7.053 nM 8.15
CHEMBL3648334 IC50 = 8.428 nM 8.07
CHEMBL3648341 IC50 = 10.07 nM 8.00
CHEMBL3648334 IC50 = 12.79 nM 7.89
CHEMBL3648330 IC50 = 12.92 nM 7.89
CHEMBL3648333 IC50 = 13.76 nM 7.86
CHEMBL3648340 IC50 = 16.18 nM 7.79
CHEMBL3648341 IC50 = 17.96 nM 7.75
CHEMBL3648340 IC50 = 18.28 nM 7.74
CHEMBL3648328 IC50 = 21.82 nM 7.66
CHEMBL3648339 IC50 = 28.99 nM 7.54
CHEMBL3648338 IC50 = 33.13 nM 7.48
CHEMBL3648335 IC50 = 39.77 nM 7.40
CHEMBL3648338 IC50 = 44.4 nM 7.35
CHEMBL3648339 IC50 = 47.03 nM 7.33
CHEMBL3648336 IC50 = 51.12 nM 7.29
CHEMBL3648335 IC50 = 53.61 nM 7.27
CHEMBL4285417 CERALASERTIB IC50 = 58.34 nM 7.23
CHEMBL3648337 IC50 = 62.55 nM 7.20
CHEMBL3648337 IC50 = 70.85 nM 7.15
CHEMBL3648330 IC50 = 75.77 nM 7.12
CHEMBL3648332 IC50 = 109.0 nM 6.96
CHEMBL3648332 IC50 = 159.3 nM 6.80
CHEMBL3648328 IC50 = 235.5 nM 6.63
CHEMBL3648327 IC50 = 581.0 nM 6.24