Assay Detail

CHEMBL5506838

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Binding

Inhibition of ATR (unknown origin) by Morrison equation based analysis

ChEMBL ↗

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Target

Serine/threonine-protein kinase ATR (CHEMBL5024) ↗

Open DB target context

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Serine/threonine-protein kinase ATR (CHEMBL5024) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Serine/threonine-protein kinase ATR

CHEMBL5024

Anchored from Assay target.

Protein identity Serine/threonine-protein kinase ATR

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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 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
Ki	4	9.06	10.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4285417	CERALASERTIB	3.0	1	10.22
CHEMBL4650286	M4344	1.0	1	8.54
CHEMBL4647810	ELIMUSERTIB	1.0	1	8.42
CHEMBL3989870	BERZOSERTIB	2.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4285417	CERALASERTIB	Ki	=	0.06	nM	10.22
CHEMBL4650286	M4344	Ki	=	2.9	nM	8.54
CHEMBL4647810	ELIMUSERTIB	Ki	=	3.8	nM	8.42
CHEMBL3989870	BERZOSERTIB	Ki	=	0.008	nM	-