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Assay Detail

CHEMBL5506837

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

Binding
Inhibition of human ATR/ATRIP using GST-tagged p53 as substrate in presence of 3 uM ATP by AlphaScreen assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

ATR/ATRIP (CHEMBL4106138)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).
Black WC, Abdoli A, An X, Auger A, Beaulieu P, Bernatchez M, Caron C, Chefson A, Crane S, Diallo M, Dorich S, Fader LD, Ferraro GB, Fournier S, Gao Q, Ginzburg Y, Hamel M, Han Y, Jones P, Lanoix S, Lacbay CM, Leclaire ME, Levy M, Mamane Y, Mulani A, Papp R, Pellerin C, Picard A, Skeldon A, Skorey K, Stocco R, St-Onge M, Truchon JF, Truong VL, Zimmermann M, Zinda M, Roulston A.
J Med Chem (2024) 67 : 2349 -2368
PubMed 38299539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.35 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325697 1 8.30
CHEMBL5557486 1 8.15
CHEMBL4285417 CERALASERTIB 3.0 1 7.85
CHEMBL5568349 1 7.40
CHEMBL5568570 1 7.00
CHEMBL4650286 M4344 1.0 1 6.80
CHEMBL5556905 1 6.80
CHEMBL4647810 ELIMUSERTIB 1.0 1 6.48
CHEMBL3989870 BERZOSERTIB 2.0 1 -
CHEMBL5518146 1 -
CHEMBL5557127 1 -
CHEMBL5532160 1 -
CHEMBL5564966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325697 IC50 = 5.0 nM 8.30
CHEMBL5557486 IC50 = 7.0 nM 8.15
CHEMBL4285417 CERALASERTIB IC50 = 14.0 nM 7.85
CHEMBL5568349 IC50 = 40.0 nM 7.40
CHEMBL5568570 IC50 = 100.0 nM 7.00
CHEMBL4650286 M4344 IC50 = 160.0 nM 6.80
CHEMBL5556905 IC50 = 160.0 nM 6.80
CHEMBL4647810 ELIMUSERTIB IC50 = 330.0 nM 6.48
CHEMBL3989870 BERZOSERTIB IC50 < 1.0 nM -
CHEMBL5518146 IC50 > 1000.0 nM -
CHEMBL5557127 IC50 > 1000.0 nM -
CHEMBL5532160 IC50 > 700.0 nM -
CHEMBL5564966 IC50 > 1000.0 nM -