Assay Detail

CHEMBL5506867

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Binding

Inhibition of ATR in gemcitabine-stimulated human LoVo cells assessed as decrease in CHK1 phosphorylation at Ser345 residue

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
Cell Type	LoVo
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
IC50	4	8.75	9.48

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5095260	CAMONSERTIB	2.0	1	9.48
CHEMBL4647810	ELIMUSERTIB	1.0	1	9.22
CHEMBL4650286	M4344	1.0	1	8.96
CHEMBL4285417	CERALASERTIB	3.0	1	7.33

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5095260	CAMONSERTIB	IC50	=	0.33	nM	9.48
CHEMBL4647810	ELIMUSERTIB	IC50	=	0.6	nM	9.22
CHEMBL4650286	M4344	IC50	=	1.1	nM	8.96
CHEMBL4285417	CERALASERTIB	IC50	=	47.0	nM	7.33