TargetEnzymes

Histone-lysine N-methyltransferase 2A

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements: 2
Compounds: 2
Binding constants: 0
Median pX: —

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

KMT2A_HUMANKMT2AHomo sapiens

Histone-lysine N-methyltransferase 2A

Histone methyltransferase that plays an essential role in early development and hematopoiesis12453419,15960975,19187761,19556245,20677832,21220120,26886794. Catalytic subunit of the MLL1/MLL complex, a multiprotein complex that mediates both methylation of 'Lys-4' of histone H3 (H3K4me) complex and acetylation of 'Lys-16' of histone H4 (H4K16ac)12453419,15960975,19187761,19556245,20677832,21220120,24235145,26886794. Catalyzes methyl group transfer from S-adenosyl-L-methionine to the epsilon-amino group of 'Lys-4' of histone H3 (H3K4) via a non-processive mechanism. Part of chromatin remodeling machinery predominantly forms H3K4me1 and H3K4me2 methylation marks at active chromatin sites where transcription and DNA repair take place12453419,15960975,19187761,19556245,20677832,21220120,25561738,26886794. Has weak methyltransferase activity by itself, and requires other component of the MLL1/MLL complex to obtain full methyltransferase activity19187761,26886794. Has no activity toward histone H3 phosphorylated on 'Thr-3', less activity toward H3 dimethylated on 'Arg-8' or 'Lys-9', while it has higher activity toward H3 acetylated on 'Lys-9'19187761. Binds to unmethylated CpG elements in the promoter of target genes and helps maintain them in the nonmethylated state20010842. Required for transcriptional activation of HOXA912453419,20010842,20677832. Promotes PPP1R15A-induced apoptosis10490642. Plays a critical role in the control of circadian gene expression and is essential for the transcriptional activation mediated by the CLOCK-BMAL1 heterodimer (By similarity). Establishes a permissive chromatin state for circadian transcription by mediating a rhythmic methylation of 'Lys-4' of histone H3 (H3K4me) and this histone modification directs the circadian acetylation at H3K9 and H3K14 allowing the recruitment of CLOCK-BMAL1 to chromatin (By similarity). Also has auto-methylation activity on Cys-3882 in absence of histone H3 substrate24235145

Quoted from UniProt’s FUNCTION annotation for Q03164 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

Partner	Combined	Experiment	Database	Text mining
WDR5	0.999	0.991	0.900	0.978
RBBP5	0.999	0.993	0.900	0.895
ASH2L	0.999	0.993	0.900	0.924
MEN1	0.999	0.911	0.800	0.990
KMT2D	0.997	0.335	0.900	0.954
DPY30	0.995	0.954	0.540	0.785
CREBBP	0.995	0.981	0.000	0.727
HCFC1	0.991	0.646	0.900	0.765
AFF1	0.990	0.552	0.000	0.978
H3C12	0.989	0.952	0.500	0.591

Where it sits in the cell

Nucleoplasm
Cytosoladditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Nucleus

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Functional readouts 2

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

Target	Class	Type	Value (nM)	pX	Organism	Assay
Histone-lysine N-methyltransferase 2A	Enzymes	Potency	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL1614410
Histone-lysine N-methyltransferase 2A	Enzymes	Potency	— no normalized value	— value does not convert to pX	Homo sapiens	CHEMBL1614410

← All targets