Assay Detail

CHEMBL5713136

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Binding

Inhibition of WDR5/MLL interaction in human HEK293 cells expressing FLAG-tagged human WDR5 plasmid after 5 hrs incubation by immunoprecipitation analysis

ChEMBL ↗

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Target

Histone-lysine N-methyltransferase 2A/WDR5 (CHEMBL3883320) ↗

Open DB target context

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Histone-lysine N-methyltransferase 2A/WDR5 (CHEMBL3883320) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histone-lysine N-methyltransferase 2A/WDR5

CHEMBL3883320

Anchored from Assay target.

Protein identity Histone-lysine N-methyltransferase 2A/WDR5

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	HEK293
Confidence	5 — Multiple protein complex / RNA
Curated By	Autocuration

Target

Histone-lysine N-methyltransferase 2A/WDR5 (CHEMBL3883320) ↗

Type	PROTEIN-PROTEIN INTERACTION
Organism	Homo sapiens

Publication

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.

Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D, Barsyte-Lovejoy D, Li F, Poda G, Schapira M, Wu H, Dong A, Senisterra G, Stukalov A, Huber KVM, Schönegger A, Marcellus R, Bilban M, Bock C, Brown PJ, Zuber J, Bennett KL, Al-Awar R, Delwel R, Nerlov C, Arrowsmith CH, Superti-Furga G.
Nat Chem Biol (2015) 11 : 571 -578
PubMed 26167872 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.65	6.65

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000222
EFO_ID	EFO_ID	-	—	EFO:0000222
EFO_TERM	EFO_TERM	-	—	acute myeloid leukemia
EFO_TERM	EFO_TERM	-	—	acute myeloid leukemia

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3798846	—	—	1	6.65

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3798846	—	IC50	=	223.0	nM	6.65