General Information of the Protein
Protein ID
PT02593
Protein Name
Bromodomain-containing protein 1
Secondarily
Protein Name
BR140-like protein
Bromodomain and PHD finger-containing protein 2
Gene Name
BRD1
Secondarily
Gene Name
BRL
BRPF2
Sequence
MRRKGRCHRGSAARHPSSPCSVKHSPTRETLTYAQAQRMVEIEIEGRLHRISIFDPLEIILEDDLTAQEMSECNSNKENSERPPVCLRTKRHKNNRVKKKNEALPSAHGTPASASALPEPKVRIVEYSPPSAPRRPPVYYKFIEKSAEELDNEVEYDMDEEDYAWLEIVNEKRKGDCVPAVSQSMFEFLMDRFEKESHCENQKQGEQQSLIDEDAVCCICMDGECQNSNVILFCDMCNLAVHQECYGVPYIPEGQWLCRHCLQSRARPADCVLCPNKGGAFKKTDDDRWGHVVCALWIPEVGFANTVFIEPIDGVRNIPPARWKLTCYLCKQKGVGACIQCHKANCYTAFHVTCAQKAGLYMKMEPVKELTGGGTTFSVRKTAYCDVHTPPGCTRRPLNIYGDVEMKNGVCRKESSVKTVRSTSKVRKKAKKAKKALAEPCAVLPTVCAPYIPPQRLNRIANQVAIQRKKQFVERAHSYWLLKRLSRNGAPLLRRLQSSLQSQRSSQQRENDEEMKAAKEKLKYWQRLRHDLERARLLIELLRKREKLKREQVKVEQVAMELRLTPLTVLLRSVLDQLQDKDPARIFAQPVSLKEVPDYLDHIKHPMDFATMRKRLEAQGYKNLHEFEEDFDLIIDNCMKYNARDTVFYRAAVRLRDQGGVVLRQARREVDSIGLEEASGMHLPERPAAAPRRPFSWEDVDRLLDPANRAHLGLEEQLRELLDMLDLTCAMKSSGSRSKRAKLLKKEIALLRNKLSQQHSQPLPTGPGLEGFEEDGAALGPEAGEEVLPRLETLLQPRKRSRSTCGDSEVEEESPGKRLDAGLTNGFGGARSEQEPGGGLGRKATPRRRCASESSISSSNSPLCDSSFNAPKCGRGKPALVRRHTLEDRSELISCIENGNYAKAARIAAEVGQSSMWISTDAAASVLEPLKVVWAKCSGYPSYPALIIDPKMPRVPGHHNGVTIPAPPLDVLKIGEHMQTKSDEKLFLVLFFDNKRSWQWLPKSKMVPLGIDETIDKLKMMEGRNSSIRKAVRIAFDRAMNHLSRVHGEPTSDLSDID
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
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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, that acts as a regulator of hematopoiesis (PubMed:16387653, PubMed:21753189, PubMed:21880731). Plays a key role in HBO1 complex by directing KAT7/HBO1 specificity towards histone H3 'Lys-14' acetylation (H3K14ac), thereby promoting erythroid differentiation (PubMed:21753189).
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Uniprot ID
Primary ID:
O95696

Secondarily ID:
A6ZJA4
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Ensembl ID
ENSG00000100425
HGNC ID
HGNC:1102
Subcellular Location
Nucleus
Chromosome
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: CL000067 , HCT 116
Compound ID Compound Name Compound Formula
CP0538825
6-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C30H34N6O3
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0249938
6-morpholin-4-yl-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C26H24N4O4
 1
1
IC50 = 613 nM
   TI
   LI
   LO
   TS
CP0127914
6-chloro-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C22H16ClN3O3
 1
1
IC50 = 675 nM
   TI
   LI
   LO
   TS
CP0249937
2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C27H36N2O5
 1
1
IC50 = 740 nM
   TI
   LI
   LO
   TS
CP0086064
6-(3-hydroxypropyl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C25H23N3O4
 1
1
IC50 = 825 nM
   TI
   LI
   LO
   TS
CP0139490
6-[4-(cyclopropylmethyl)piperazin-1-yl]-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C30H31N5O3
 1
1
IC50 = 863 nM
   TI
   LI
   LO
   TS
CP0127913
6-(4-methoxypiperidin-1-yl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C28H28N4O4
 1
1
IC50 = 915 nM
   TI
   LI
   LO
   TS
CP0214084
6-[methyl(2-pyrrolidin-1-ylethyl)amino]-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C29H31N5O3
 1
1
IC50 = 941 nM
   TI
   LI
   LO
   TS
CP0127912
6-(4-methylpiperazin-1-yl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C27H27N5O3
 1
1
IC50 = 1240 nM
   TI
   LI
   LO
   TS
CP0274334
2-(6-methoxy-1,3-dimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C22H17N3O4
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0072475
6-(4-hydroxypiperidin-1-yl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C27H26N4O4
 1
1
IC50 = 2120 nM
   TI
   LI
   LO
   TS
CP0127907
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 > 10000 nM
   TI
   LI
   LO
   TS
CP0127908
6-pyrrolidin-1-yl-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C26H24N4O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0127909
6-piperidin-1-yl-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C27H26N4O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0086064
6-(3-hydroxypropyl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
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C25H23N3O4
 3
1 IC50 = 45 nM
2 IC50 = 67 nM
3 IC50 = 97 nM
Clinical Information about the Protein
Target 1 ( Bromodomain-containing protein 1 (BRD1) )
Target Type Literature-reported Target