General Information of the Protein
Protein ID
PT03324
Protein Name
WD repeat-containing protein 5
Secondarily
Protein Name
BMP2-induced 3-kb gene protein
Gene Name
WDR5
Secondarily
Gene Name
BIG3
Sequence
MATEEKKPETEAARAQPTPSSSATQSKPTPVKPNYALKFTLAGHTKAVSSVKFSPNGEWLASSSADKLIKIWGAYDGKFEKTISGHKLGISDVAWSSDSNLLVSASDDKTLKIWDVSSGKCLKTLKGHSNYVFCCNFNPQSNLIVSGSFDESVRIWDVKTGKCLKTLPAHSDPVSAVHFNRDGSLIVSSSYDGLCRIWDTASGQCLKTLIDDDNPPVSFVKFSPNGKYILAATLDNTLKLWDYSKGKCLKTYTGHKNEKYCIFANFSVTGGKWIVSGSEDNLVYIWNLQTKEIVQKLQGHTDVVISTACHPTENIIASAALENDKTIKLWKSDC
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Organism
Homo sapiens, Human
Protein Classification
Other nuclear protein
Function
Contributes to histone modification (PubMed:19131338, PubMed:19556245, PubMed:19103755, PubMed:20018852, PubMed:16600877, PubMed:16829960). May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4' (PubMed:16829960). As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3 (PubMed:19556245). H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation (PubMed:18840606). As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues (PubMed:19103755, PubMed:20018852). May regulate osteoblasts differentiation (By similarity). In association with RBBP5 and ASH2L, stimulates the histone methyltransferase activities of KMT2A, KMT2B, KMT2C, KMT2D, SETD1A and SETD1B (PubMed:21220120, PubMed:22266653).
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Uniprot ID
Primary ID:
P61964

Secondarily ID:
Q91VA5
Q9NWX7
Q9UGP9
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HGNC ID
HGNC:12757
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: CL000017 , HeLa
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0472253
 Compound Info 
N-[(1R)-6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl]-3,5-dimethoxy-4-methylbenzamide
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C25H27N3O3
  1
1
IC50 = 3200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0482343
 Compound Info 
2-(3,4-dichlorophenyl)-N-[(1R)-6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl]acetamide
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C23H21Cl2N3O
  1
1
IC50 = 9270 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0451026
 Compound Info 
N-[(1R)-6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl]-2-(3-methoxy-4-methylphenyl)acetamide
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C25H27N3O2
  1
1
IC50 = 12000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0482344
 Compound Info 
N-[(1R)-7-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]-3-methoxy-4-methylbenzamide
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C25H27N3O2
  1
1
IC50 > 20000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0552451
 Compound Info 
N-[(1R)-6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl]-2-methylpyridine-4-carboxamide
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C22H22N4O
  1
1
IC50 > 20000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0273253
 Compound Info 
N-[5-[4-[[5-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-5-oxopentyl]carbamoyl]phenyl]-2-(4-methylpiperazin-1-yl)phenyl]-6-oxo-4-(trifluoromethyl)-1H-pyridine-3-carboxamide
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C52H60F3N9O7S
  1
1 Kd = 18 nM
CP0152799
 Compound Info 
2-chloro-N-[2-(4-methylpiperazin-1-yl)-5-nitrophenyl]benzamide
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C18H19ClN4O3
  3
1 Kd = 4000 nM
2 Kd = 7000 nM
3 Kd = 12000 nM
Clinical Information about the Protein
Target 1 ( WD repeat-containing protein 5 (WDR5) )
Target Type Literature-reported Target