General Information of the Protein
Protein ID
PT02678
Protein Name
Histone-lysine N-methyltransferase, H3 lysine-79 specific
Secondarily
Protein Name
DOT1-like protein
Histone H3-K79 methyltransferase
Lysine N-methyltransferase 4
Gene Name
DOT1L
Secondarily
Gene Name
KIAA1814
KMT4
Sequence
MGEKLELRLKSPVGAEPAVYPWPLPVYDKHHDAAHEIIETIRWVCEEIPDLKLAMENYVLIDYDTKSFESMQRLCDKYNRAIDSIHQLWKGTTQPMKLNTRPSTGLLRHILQQVYNHSVTDPEKLNNYEPFSPEVYGETSFDLVAQMIDEIKMTDDDLFVDLGSGVGQVVLQVAAATNCKHHYGVEKADIPAKYAETMDREFRKWMKWYGKKHAEYTLERGDFLSEEWRERIANTSVIFVNNFAFGPEVDHQLKERFANMKEGGRIVSSKPFAPLNFRINSRNLSDIGTIMRVVELSPLKGSVSWTGKPVSYYLHTIDRTILENYFSSLKNPKLREEQEAARRRQQRESKSNAATPTKGPEGKVAGPADAPMDSGAEEEKAGAATVKKPSPSKARKKKLNKKGRKMAGRKRGRPKKMNTANPERKPKKNQTALDALHAQTVSQTAASSPQDAYRSPHSPFYQLPPSVQRHSPNPLLVAPTPPALQKLLESFKIQYLQFLAYTKTPQYKASLQELLGQEKEKNAQLLGAAQQLLSHCQAQKEEIRRLFQQKLDELGVKALTYNDLIQAQKEISAHNQQLREQSEQLEQDNRALRGQSLQLLKARCEELQLDWATLSLEKLLKEKQALKSQISEKQRHCLELQISIVELEKSQRQQELLQLKSCVPPDDALSLHLRGKGALGRELEPDASRLHLELDCTKFSLPHLSSMSPELSMNGQAAGYELCGVLSRPSSKQNTPQYLASPLDQEVVPCTPSHVGRPRLEKLSGLAAPDYTRLSPAKIVLRRHLSQDHTVPGRPAASELHSRAEHTKENGLPYQSPSVPGSMKLSPQDPRPLSPGALQLAGEKSSEKGLRERAYGSSGELITSLPISIPLSTVQPNKLPVSIPLASVVLPSRAERARSTPSPVLQPRDPSSTLEKQIGANAHGAGSRSLALAPAGFSYAGSVAISGALAGSPASLTPGAEPATLDESSSSGSLFATVGSRSSTPQHPLLLAQPRNSLPASPAHQLSSSPRLGGAAQGPLPEASKGDLPSDSGFSDPESEAKRRIVFTITTGAGSAKQSPSSKHSPLTASARGDCVPSHGQDSRRRGRRKRASAGTPSLSAGVSPKRRALPSVAGLFTQPSGSPLNLNSMVSNINQPLEITAISSPETSLKSSPVPYQDHDQPPVLKKERPLSQTNGAHYSPLTSDEEPGSEDEPSSARIERKIATISLESKSPPKTLENGGGLAGRKPAPAGEPVNSSKWKSTFSPISDIGLAKSADSPLQASSALSQNSLFTFRPALEEPSADAKLAAHPRKGFPGSLSGADGLSPGTNPANGCTFGGGLAADLSLHSFSDGASLPHKGPEAAGLSSPLSFPSQRGKEGSDANPFLSKRQLDGLAGLKGEGSRGKEAGEGGLPLCGPTDKTPLLSGKAAKARDREVDLKNGHNLFISAAAVPPGSLLSGPGLAPAASSAGGAASSAQTHRSFLGPFPPGPQFALGPMSLQANLGSVAGSSVLQSLFSSVPAAAGLVHVSSAATRLTNSHAMGSFSGVAGGTVGGN
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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Writer
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Protein methyltransferase
Function
Histone methyltransferase. Methylates 'Lys-79' of histone H3. Nucleosomes are preferred as substrate compared to free histones (PubMed:12123582). Binds to DNA (PubMed:12628190).
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Uniprot ID
Primary ID:
Q8TEK3

Secondarily ID:
O60379
Q96JL1
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Ensembl ID
ENSG00000104885
HGNC ID
HGNC:24948
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000091 , MV4-11
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0416983
 Compound Info 
6-(1,3-benzodioxol-5-yl)-3-(benzotriazol-1-ylmethyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C17H11N7O2S
  1
1
IC50 = 6750 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0567136
 Compound Info 
3-(benzotriazol-1-ylmethyl)-6-(4-fluorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C16H10FN7S
  1
1
IC50 = 8000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0465737
 Compound Info 
3-(benzotriazol-1-ylmethyl)-6-(4-tert-butylphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C20H19N7S
  1
1
IC50 = 13050 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0320291
 Compound Info 
3-(benzotriazol-1-ylmethyl)-6-(3-fluorophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C16H10FN7S
  1
1
IC50 = 21910 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0441205
 Compound Info 
3-(benzimidazol-1-ylmethyl)-6-(3-bromophenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C17H11BrN6S
  1
1
IC50 = 26780 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0570203
 Compound Info 
1-{[6-(2,3-dihydro-1,4-benzodioxin-6-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl]methyl}-1H-1,2,3-benzotriazole
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C18H13N7O2S
  1
1
IC50 = 40730 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0260316
 Compound Info 
3-(1-benzotriazolylmethyl)-6-(phenylmethyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C17H13N7S
  1
1
IC50 = 48800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0566569
 Compound Info 
3-(benzimidazol-1-ylmethyl)-6-(3,4-dimethylphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C19H16N6S
  1
1
IC50 = 63970 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0478449
 Compound Info 
3-(benzotriazol-1-ylmethyl)-6-(3-methoxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
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C17H13N7OS
  1
1
IC50 = 64150 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000040 , THP-1
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0093774
 Compound Info 
CHEMBL3414626
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C30H42N8O3
  4
1 IC50 < 0.1 nM
2 IC50 = 0.74 nM
3 Ki = 0.012 nM
4 Ki = 0.08 nM
CP0126272
 Compound Info 
2-[[2-chloro-3-(2-methylpyridin-3-yl)-1-benzothiophen-5-yl]carbamoylamino]-N-[3-[methyl-[(3R)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-3-yl]amino]propyl]acetamide
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C32H36ClN9O2S
  1
1 IC50 < 0.1 nM
CP0467968
 Compound Info 
3-[(4-amino-6-methoxy-1,3,5-triazin-2-yl)amino]-4-[[(S)-(3-chloropyridin-2-yl)-(2,2-difluoro-1,3-benzodioxol-4-yl)methyl]amino]benzenesulfonamide
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C23H19ClF2N8O5S
  1
1 IC50 = 0.17 nM
CP0437957
 Compound Info 
1-N-[(S)-(3-chloropyridin-2-yl)-(2,2-difluoro-1,3-benzodioxol-4-yl)methyl]-2-N-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylsulfonylbenzene-1,2-diamine
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C25H21ClF2N6O6S
  1
1 IC50 = 0.19 nM
CP0369305
 Compound Info 
1-[3-[[(2R,3S,4R,5R)-5-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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C28H40BrN7O4
  2
1 IC50 = 0.3 nM
2 Kd = 0.06 nM
CP0010318
 Compound Info 
1-[3-[[(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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C28H41N7O4
  3
1 IC50 = 0.4 nM
2 Kd = 0.25 nM
3 Ki = 0.3 nM
CP0150612
 Compound Info 
4-N-methyl-2-N-[2-methyl-1-[2-(3-methylimidazo[4,5-b]pyridin-6-yl)oxyphenyl]indol-6-yl]pyrimidine-2,4-diamine
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C27H24N8O
  2
1 IC50 = 0.4 nM
2 Ki = 0.08 nM
CP0536309
 Compound Info 
1-N-[(S)-(3-chloro-2-fluorophenyl)-(3-fluoropyridin-2-yl)methyl]-2-N-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylsulfonylbenzene-1,2-diamine
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C24H21ClF2N6O4S
  1
1 IC50 = 0.59 nM
CP0355612
 Compound Info 
2-[2-[[(S)-(3-chloro-2-fluorophenyl)-pyridin-2-ylmethyl]amino]-5-methylsulfonylanilino]pyrimidine-4-carboxamide
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C24H20ClFN6O3S
  2
1 IC50 = 2.1 nM
2 IC50 = 3.9 nM
CP0150611
 Compound Info 
5-[6-chloro-5-[2-chloro-5-[[4-(methylamino)pyrimidin-2-yl]amino]-1-benzothiophen-3-yl]pyridin-3-yl]-3,6-dimethylpyrimidin-4-one
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C24H19Cl2N7OS
  2
1 IC50 = 1400 nM
2 Ki = 0.36 nM
CP0011023
 Compound Info 
AdoHcy
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C14H20N6O5S
  4
1 Kd = 150 nM
2 Kd = 360 nM
3 Ki = 160 nM
4 Ki = 270 nM
Clinical Information about the Protein
Target 1 ( Histone-lysine N-methyltransferase (HLNM) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Acute myeloid leukaemia [ICD-11: 2A60]
2 leukaemia [ICD-11: 2A60-2B33]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 EPZ-5676
 Drug Info 
Phase 1/2
Acute myeloid leukaemia
Investigative Drug(s) 1 Investigative Drug  1
1 EPZ-004777
 Drug Info 
Investigative
leukaemia