Assay Detail

CHEMBL5657788

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Binding

Inhibition of human ERK8 in presence of ATP by by radiometric kinase assay

ChEMBL ↗

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Target

Mitogen-activated protein kinase 15 (CHEMBL5198) ↗

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Mitogen-activated protein kinase 15 (CHEMBL5198) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Mitogen-activated protein kinase 15

CHEMBL5198

Anchored from Assay target.

Protein identity Mitogen-activated protein kinase 15

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

Mitogen-activated protein kinase 15 (CHEMBL5198) ↗

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	6.89	6.89

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	6.89

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4169078	SRA-737	IC50	=	130.0	nM	6.89