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Assay Detail

CHEMBL5506832

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

Binding
Inhibition of human full length recombinant ATR M211T mutant using GST-c-Myc-p53 as substrate measured after 30 mins in presence of Mg/ATP mix by ELISA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 3 7.72 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3989870 BERZOSERTIB 2.0 1 8.30
CHEMBL2325697 1 8.00
CHEMBL4285417 CERALASERTIB 3.0 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3989870 BERZOSERTIB IC50 = 5.0 nM 8.30
CHEMBL2325697 IC50 = 10.0 nM 8.00
CHEMBL4285417 CERALASERTIB IC50 = 134.0 nM 6.87