Assay Detail

CHEMBL4324299

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Binding

Inhibition of recombinant full length human His-tagged ARK5 expressed in baculovirus expression system

ChEMBL ↗

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Target

NUAK family SNF1-like kinase 1 (CHEMBL5784) ↗

Open DB target context

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NUAK family SNF1-like kinase 1 (CHEMBL5784) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target NUAK family SNF1-like kinase 1

CHEMBL5784

Anchored from Assay target.

Protein identity NUAK family SNF1-like kinase 1

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

NUAK family SNF1-like kinase 1 (CHEMBL5784) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).

Ward RA, Anderton MJ, Bethel P, Breed J, Cook C, Davies EJ, Dobson A, Dong Z, Fairley G, Farrington P, Feron L, Flemington V, Gibbons FD, Graham MA, Greenwood R, Hanson L, Hopcroft P, Howells R, Hudson J, James M, Jones CD, Jones CR, Li Y, Lamont S, Lewis R, Lindsay N, McCabe J, McGuire T, Rawlins P, Roberts K, Sandin L, Simpson I, Swallow S, Tang J, Tomkinson G, Tonge M, Wang Z, Zhai B.
J Med Chem (2019) 62 : 11004 -11018
PubMed 31710489 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.40	6.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4482864	TIZATERKIB	1.0	1	6.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4482864	TIZATERKIB	IC50	=	400.0	nM	6.40