General Information of the Protein
Protein ID
PT02995
Protein Name
Peregrin
Secondarily
Protein Name
Bromodomain and PHD finger-containing protein 1
Protein Br140
Gene Name
BRPF1
Secondarily
Gene Name
BR140
Sequence
MGVDFDVKTFCHNLRATKPPYECPVETCRKVYKSYSGIEYHLYHYDHDNPPPPQQTPLRKHKKKGRQSRPANKQSPSPSEVSQSPGREVMSYAQAQRMVEVDLHGRVHRISIFDNLDVVSEDEEAPEEAPENGSNKENTETPAATPKSGKHKNKEKRKDSNHHHHHNVSASTTPKLPEVVYRELEQDTPDAPPRPTSYYRYIEKSAEELDEEVEYDMDEEDYIWLDIMNERRKTEGVSPIPQEIFEYLMDRLEKESYFESHNKGDPNALVDEDAVCCICNDGECQNSNVILFCDMCNLAVHQECYGVPYIPEGQWLCRRCLQSPSRAVDCALCPNKGGAFKQTDDGRWAHVVCALWIPEVCFANTVFLEPIDSIEHIPPARWKLTCYICKQRGSGACIQCHKANCYTAFHVTCAQQAGLYMKMEPVRETGANGTSFSVRKTAYCDIHTPPGSARRLPALSHSEGEEDEDEEEDEGKGWSSEKVKKAKAKSRIKMKKARKILAEKRAAAPVVSVPCIPPHRLSKITNRLTIQRKSQFMQRLHSYWTLKRQSRNGVPLLRRLQTHLQSQRNCDQVGRDSEDKNWALKEQLKSWQRLRHDLERARLLVELIRKREKLKRETIKVQQIAMEMQLTPFLILLRKTLEQLQEKDTGNIFSEPVPLSEVPDYLDHIKKPMDFFTMKQNLEAYRYLNFDDFEEDFNLIVSNCLKYNAKDTIFYRAAVRLREQGGAVLRQARRQAEKMGIDFETGMHIPHSLAGDEATHHTEDAAEEERLVLLENQKHLPVEEQLKLLLERLDEVNASKQSVGRSRRAKMIKKEMTALRRKLAHQRETGRDGPERHGPSSRGSLTPHPAACDKDGQTDSAAEESSSQETSKGLGPNMSSTPAHEVGRRTSVLFSKKNPKTAGPPKRPGRPPKNRESQMTPSHGGSPVGPPQLPIMSSLRQRKRGRSPRPSSSSDSDSDKSTEDPPMDLPANGFSGGNQPVKKSFLVYRNDCSLPRSSSDSESSSSSSSSAASDRTSTTPSKQGRGKPSFSRGTFPEDSSEDTSGTENEAYSVGTGRGVGHSMVRKSLGRGAGWLSEDEDSPLDALDLVWAKCRGYPSYPALIIDPKMPREGMFHHGVPIPVPPLEVLKLGEQMTQEAREHLYLVLFFDNKRTWQWLPRTKLVPLGVNQDLDKEKMLEGRKSNIRKSVQIAYHRALQHRSKVQGEQSSETSDSD
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Reader
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Methyl-lysine/arginine binding protein
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PWWP domain
Function
Scaffold subunit of various histone acetyltransferase (HAT) complexes, such as the MOZ/MORF and HBO1 complexes, which have a histone H3 acetyltransferase activity (PubMed:16387653, PubMed:24065767, PubMed:27939640). Plays a key role in HBO1 complex by directing KAT7/HBO1 specificity towards histone H3 'Lys-14' acetylation (H3K14ac) (PubMed:24065767). Some HAT complexes preferentially mediate histone H3 'Lys-23' (H3K23ac) acetylation (PubMed:27939640). Positively regulates the transcription of RUNX1 and RUNX2 (PubMed:18794358).
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Uniprot ID
Primary ID:
P55201

Secondarily ID:
B4DEZ6
Q7Z6E0
Q8TCM6
Q9UHI0
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Ensembl ID
ENSG00000156983
HGNC ID
HGNC:14255
Subcellular Location
Nucleus
Chromosome
Cytoplasm
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: CL000059 , HuT 78
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0717935
 Compound Info 
rac-8-(((3R,4R)-3-((1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-methoxy)piperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)quinolin-2(1H)-one
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C27H34N4O4S
  1
1
Kd = 25118.86 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0199056
 Compound Info 
8-[[(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one
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C27H35N5O2
  1
1
Kd > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0651910
 Compound Info 
8-(((3R,4R)-3-((1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-methoxy)-1-methylpiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one
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C27H35N5O4S
  1
1
Kd > 100000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000067 , HCT 116
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0274334
 Compound Info 
2-(6-methoxy-1,3-dimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C22H17N3O4
  1
1 IC50 = 1150 nM
CP0249937
 Compound Info 
2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C27H36N2O5
  1
1 IC50 = 1550 nM
CP0086064
 Compound Info 
6-(3-hydroxypropyl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C25H23N3O4
  2
1 IC50 = 2280 nM
2 IC50 = 3150 nM
CP0127907
 Compound Info 
6-(3-hydroxypropyl)-2-(1-methyl-2-oxo-3H-benzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C23H19N3O4
  1
1 IC50 > 20000 nM
CP0181513
 Compound Info 
N-[1,3-dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide
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C22H27N5O3
  1
1 Kd = 0.3162 nM
CP0651910
 Compound Info 
8-(((3R,4R)-3-((1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-methoxy)-1-methylpiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one
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C27H35N5O4S
  1
1 Ki = 5011.87 nM
Clinical Information about the Protein
Target 1 ( Bromodomain and PHD finger containing 1 (BRPF1) )
Target Type Literature-reported Target