Assay Detail

CHEMBL5657823

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Binding

Inhibition of CHK1 in etoposide-induced human MIA PaCa-2 cells assessed as G2 checkpoint abrogation in presence of nocodazole by ELISA analysis

ChEMBL ↗

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Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗

Open DB target context

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Serine/threonine-protein kinase Chk1 (CHEMBL4630) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Serine/threonine-protein kinase Chk1

CHEMBL4630

Anchored from Assay target.

Protein identity Serine/threonine-protein kinase Chk1

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	MIA PaCa-2
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.

Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, Perkins ND, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Collins I, Garrett MD.
Oncotarget (2016) 7 : 2329 -2342
PubMed 26295308 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.20	7.20

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:1001938
EFO_TERM	EFO_TERM	-	—	b-cell non-hodgkins lymphoma

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4169078	SRA-737	1.0	1	7.20

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4169078	SRA-737	IC50	=	63.0	nM	7.20