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Assay Detail

CHEMBL5576163

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

Binding
Inhibition of ATR (unknown origin)
5
Total Activities
5
Compounds Tested
2
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

Discovery of the first ataxia telangiectasia and Rad3-related (ATR) degraders for cancer treatment.
Huang L, Shao J, Lai W, Gu H, Yang J, Shi S, Wufoyrwoth S, Song Z, Zou Y, Xu Y, Zhu Q.
Eur J Med Chem (2024) 267 : 116159 -116159
PubMed 38325007 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 9.19 9.82
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4650286 M4344 1.0 1 9.82
CHEMBL3989870 BERZOSERTIB 2.0 1 9.77
CHEMBL4285417 CERALASERTIB 3.0 1 9.00
CHEMBL4647810 ELIMUSERTIB 1.0 1 8.15
CHEMBL5593857 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4650286 M4344 IC50 = 0.15 nM 9.82
CHEMBL3989870 BERZOSERTIB IC50 = 0.17 nM 9.77
CHEMBL4285417 CERALASERTIB IC50 = 1.0 nM 9.00
CHEMBL4647810 ELIMUSERTIB IC50 = 7.0 nM 8.15
CHEMBL5593857 Inhibition - % -