Assay Detail

CHEMBL5709284

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Binding

Inhibition of full length human SETD7 (1 to 366 residues) expressed in Escherichia coli BL21 (DE3) V2R-pRARE assessed as apparent inhibition constant using biotinylated H3 (1-25) peptide as substrate incubated for 1 hrs in presence of 3H-SAM by morrison equation

ChEMBL ↗

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Target

Histone-lysine N-methyltransferase SETD7 (CHEMBL5523) ↗

Open DB target context

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Loading context

Histone-lysine N-methyltransferase SETD7 (CHEMBL5523) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Histone-lysine N-methyltransferase SETD7

CHEMBL5523

Anchored from Assay target.

Protein identity Histone-lysine N-methyltransferase SETD7

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

Histone-lysine N-methyltransferase SETD7 (CHEMBL5523) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.

Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH.
Proc Natl Acad Sci U S A (2014) 111 : 12853 -12858
PubMed 25136132 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.48	9.48

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_TERM	EFO_TERM	-	—	cancer

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3414622	—	—	1	9.48

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3414622	—	Ki	=	0.33	nM	9.48