ChEMBL logo


ChEMBL Statistics
  Loading Statistics...

Target Report Card

Target Name and Classification

Target ID CHEMBL1293299
Preferred Name Histone-lysine N-methyltransferase MLL
Synonyms ALL-1 | ALL1 | C-terminal cleavage product of 180 kDa | CXXC-type zinc finger protein 7 | CXXC7 | HRX | HTRX | Histone-lysine N-methyltransferase 2A | KMT2A | Lysine N-methyltransferase 2A | MLL cleavage product C180 | MLL cleavage product N320 | MLL | MLL1 | Myeloid/lymphoid or mixed-lineage leukemia protein 1 | Myeloid/lymphoid or mixed-lineage leukemia | N-terminal cleavage product of 320 kDa | TRX1 | Trithorax-like protein | Zinc finger protein HRX | p180 | p320
Organism Homo sapiens
Species Group No
Protein Target Classification
  • epigenetic regulator > writer > protein methyltransferase
  • epigenetic regulator > reader > plant homeodomain
  • epigenetic regulator > reader > bromodomain

Target Components

Component Description Relationship Accession
Histone-lysine N-methyltransferase 2A SINGLE PROTEIN Q03164

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2093861 Menin/Histone-lysine N-methyltransferase MLL PROTEIN-PROTEIN INTERACTION
CHEMBL3883320 Histone-lysine N-methyltransferase 2A/WDR5 PROTEIN-PROTEIN INTERACTION

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000118058
Ensembl ENSG00000118058
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005829 (cytosol)
GO:0035097 (histone methyltransferase complex)
GO:0071339 (MLL1 complex)
GO Molecular Function GO:0000981 (RNA polymerase II transcription factor activity, sequence-specific DNA binding)
GO:0001046 (core promoter sequence-specific DNA binding)
GO:0003677 (DNA binding)
GO:0003680 (AT DNA binding)
GO:0003682 (chromatin binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0005515 (protein binding)
GO:0008168 (methyltransferase activity)
GO:0008270 (zinc ion binding)
GO:0016740 (transferase activity)
GO:0018024 (histone-lysine N-methyltransferase activity)
GO:0042800 (histone methyltransferase activity (H3-K4 specific))
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0044212 (transcription regulatory region DNA binding)
GO:0045322 (unmethylated CpG binding)
GO:0046872 (metal ion binding)
GO:0070577 (lysine-acetylated histone binding)
GO Biological Process GO:0006306 (DNA methylation)
GO:0006325 (chromatin organization)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006366 (transcription from RNA polymerase II promoter)
GO:0006915 (apoptotic process)
GO:0008285 (negative regulation of cell proliferation)
GO:0008542 (visual learning)
GO:0009416 (response to light stimulus)
GO:0009791 (post-embryonic development)
GO:0009952 (anterior/posterior pattern specification)
GO:0010468 (regulation of gene expression)
GO:0018026 (peptidyl-lysine monomethylation)
GO:0032259 (methylation)
GO:0032411 (positive regulation of transporter activity)
GO:0032922 (circadian regulation of gene expression)
GO:0035162 (embryonic hemopoiesis)
GO:0035640 (exploration behavior)
GO:0035864 (response to potassium ion)
GO:0043984 (histone H4-K16 acetylation)
GO:0044648 (histone H3-K4 dimethylation)
GO:0045652 (regulation of megakaryocyte differentiation)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0048172 (regulation of short-term neuronal synaptic plasticity)
GO:0048511 (rhythmic process)
GO:0048536 (spleen development)
GO:0048873 (homeostasis of number of cells within a tissue)
GO:0050890 (cognition)
GO:0051568 (histone H3-K4 methylation)
GO:0051569 (regulation of histone H3-K4 methylation)
GO:0051571 (positive regulation of histone H3-K4 methylation)
GO:0051899 (membrane depolarization)
GO:0060216 (definitive hemopoiesis)
GO:0065003 (protein-containing complex assembly)
GO:0071440 (regulation of histone H3-K14 acetylation)
GO:0080182 (histone H3-K4 trimethylation)
GO:1901674 (regulation of histone H3-K27 acetylation)
GO:1902036 (regulation of hematopoietic stem cell differentiation)
GO:1905642 (negative regulation of DNA methylation)
GO:2000615 (regulation of histone H3-K9 acetylation)
GO:2001040 (positive regulation of cellular response to drug)
Wikipedia MLL_(gene)

Target Cross References - Protein

canSAR Q03164
Human Protein Atlas ENSG00000118058
IntAct Q03164
Open Targets ENSG00000118058
PharmGKB PA241
Reactome R-HSA-3214841 (PKMTs methylate histone lysines.)
R-HSA-8936459 (RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function.)
R-HSA-8939236 (RUNX1 regulates transcription of genes involved in differentiation of HSCs.)
UniProt E9PQG7 Q03164 Q13743 Q13744 Q14845 Q16364 Q59FF2 Q6UBD1 Q9HBJ3 Q9UD94 Q9UMA3

Target Cross References - Domain

InterPro IPR001214 (SET_dom.)
IPR001487 (Bromodomain.)
IPR001965 (Znf_PHD.)
IPR002857 (Znf_CXXC.)
IPR003616 (Post-SET_dom.)
IPR003888 (FYrich_N.)
IPR003889 (FYrich_C.)
IPR011011 (Znf_FYVE_PHD.)
IPR013083 (Znf_RING/FYVE/PHD.)
IPR016569 (MeTrfase_trithorax.)
IPR019787 (Znf_PHD-finger.)
IPR034732 (EPHD.)
IPR036427 (Bromodomain-like_sf.)
Pfam PF00628 (PHD)
PF00856 (SET)
PF02008 (zf-CXXC)
PF05964 (FYRN)
PF05965 (FYRC)

Target Cross References - Structure

PDBe 2W5Y 2W5Z 3EG6 3EMH 3LQH 3LQI 3LQJ 3P4F 3U85 3U88 4ESG 4GQ6 4NW3 5F5E 5F6L
CREDO 2W5Y 2W5Z 3EG6 3EMH 3LQH 3LQI 3LQJ 3P4F 3U85 3U88 4ESG 4GQ6 4NW3 5F5E 5F6L