Assay Detail

CHEMBL4380979

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Binding

Inhibition of MNK2 (unknown origin)

ChEMBL ↗

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Target

MAP kinase-interacting serine/threonine-protein kinase 2 (CHEMBL4204) ↗

Open DB target context

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MAP kinase-interacting serine/threonine-protein kinase 2 (CHEMBL4204) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target MAP kinase-interacting serine/threonine-protein kinase 2

CHEMBL4204

Anchored from Assay target.

Protein identity MAP kinase-interacting serine/threonine-protein kinase 2

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

MAP kinase-interacting serine/threonine-protein kinase 2 (CHEMBL4204) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2.

Kwiatkowski J, Liu B, Pang S, Ahmad NHB, Wang G, Poulsen A, Yang H, Poh YR, Tee DHY, Ong E, Retna P, Dinie N, Kwek P, Wee JLK, Manoharan V, Low CB, Seah PG, Pendharkar V, Sangthongpitag K, Joy J, Baburajendran N, Jansson AE, Nacro K, Hill J, Keller TH, Hung AW.
J Med Chem (2020) 63 : 621 -637
PubMed 31910010 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	7.33	7.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL574738	AST-487	1.0	1	7.70
CHEMBL3545307	MERESTINIB	2.0	1	6.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL574738	AST-487	IC50	=	20.0	nM	7.70
CHEMBL3545307	MERESTINIB	IC50	=	109.0	nM	6.96