General Information of the Protein
Protein ID
PT03336
Protein Name
Lysine-specific histone demethylase 2
Secondarily
Protein Name
Flavin-containing amine oxidase domain-containing protein 1
Lysine-specific histone demethylase 1B
Gene Name
KDM1B
Secondarily
Gene Name
AOF1
C6orf193
LSD2
Sequence
MATPRGRTKKKASFDHSPDSLPLRSSGRQAKKKATETTDEDEDGGSEKKYRKCEKAGCTATCPVCFASASERCAKNGYTSRWYHLSCGEHFCNECFDHYYRSHKDGYDKYTTWKKIWTSNGKTEPSPKAFMADQQLPYWVQCTKPECRKWRQLTKEIQLTPQIAKTYRCGMKPNTAIKPETSDHCSLPEDLRVLEVSNHWWYSMLILPPLLKDSVAAPLLSAYYPDCVGMSPSCTSTNRAAATGNASPGKLEHSKAALSVHVPGMNRYFQPFYQPNECGKALCVRPDVMELDELYEFPEYSRDPTMYLALRNLILALWYTNCKEALTPQKCIPHIIVRGLVRIRCVQEVERILYFMTRKGLINTGVLSVGADQYLLPKDYHNKSVIIIGAGPAGLAAARQLHNFGIKVTVLEAKDRIGGRVWDDKSFKGVTVGRGAQIVNGCINNPVALMCEQLGISMHKFGERCDLIQEGGRITDPTIDKRMDFHFNALLDVVSEWRKDKTQLQDVPLGEKIEEIYKAFIKESGIQFSELEGQVLQFHLSNLEYACGSNLHQVSARSWDHNEFFAQFAGDHTLLTPGYSVIIEKLAEGLDIQLKSPVQCIDYSGDEVQVTTTDGTGYSAQKVLVTVPLALLQKGAIQFNPPLSEKKMKAINSLGAGIIEKIALQFPYRFWDSKVQGADFFGHVPPSASKRGLFAVFYDMDPQKKHSVLMSVIAGEAVASVRTLDDKQVLQQCMATLRELFKEQEVPDPTKYFVTRWSTDPWIQMAYSFVKTGGSGEAYDIIAEDIQGTVFFAGEATNRHFPQTVTGAYLSGVREASKIAAF
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Eraser
>
Lysine demethylase
>
Lysine-specific demethylase
Function
Histone demethylase that demethylates 'Lys-4' of histone H3, a specific tag for epigenetic transcriptional activation, thereby acting as a corepressor. Required for de novo DNA methylation of a subset of imprinted genes during oogenesis. Acts by oxidizing the substrate by FAD to generate the corresponding imine that is subsequently hydrolyzed. Demethylates both mono- and di-methylated 'Lys-4' of histone H3. Has no effect on tri-methylated 'Lys-4', mono-, di- or tri-methylated 'Lys-9', mono-, di- or tri-methylated 'Lys-27', mono-, di- or tri-methylated 'Lys-36' of histone H3, or on mono-, di- or tri-methylated 'Lys-20' of histone H4. Alone, it is unable to demethylate H3K4me on nucleosomes and requires the presence of GLYR1 to achieve such activity, they form a multifunctional enzyme complex that modifies transcribed chromatin and facilitates Pol II transcription through nucleosomes (PubMed:30970244).
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Uniprot ID
Primary ID:
Q8NB78

Secondarily ID:
A2A2C5
A2A2C6
Q5TGV3
Q6AI15
Q6ZUU4
Q8N258
Q96EL7
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Ensembl ID
ENSG00000165097
HGNC ID
HGNC:21577
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0551542
(1R,2R)-2-(4-bromo-3,5-difluorophenyl)cyclopropan-1-amine
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C9H8BrF2N
 1
1
Ki = 7000 nM
   TI
   LI
   LO
   TS
CP0569245
(1R,2R)-2-[2,5-difluoro-4-(3-methoxyphenyl)phenyl]cyclopropan-1-amine
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C16H15F2NO
 1
1
Ki = 7000 nM
   TI
   LI
   LO
   TS
CP0543027
(1R,2R)-2-(4-bromo-2,5-difluorophenyl)cyclopropan-1-amine
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C9H8BrF2N
 1
1
Ki = 8400 nM
   TI
   LI
   LO
   TS
CP0569642
(1R,2R)-2-(4-bromo-2,3-difluorophenyl)cyclopropan-1-amine
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C9H8BrF2N
 1
1
Ki = 17000 nM
   TI
   LI
   LO
   TS
CP0574479
(1R,2R)-2-(4-bromo-2-chloro-5-fluorophenyl)cyclopropan-1-amine
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C9H8BrClFN
 1
1
Ki = 20000 nM
   TI
   LI
   LO
   TS
CP0567978
(1R,2R)-2-(4-bromo-2-fluorophenyl)cyclopropan-1-amine
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C9H9BrFN
 1
1
Ki = 29000 nM
   TI
   LI
   LO
   TS
CP0574465
(1R,2R)-2-(4-chloro-2,5-difluorophenyl)cyclopropan-1-amine
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C9H8ClF2N
 1
1
Ki = 35000 nM
   TI
   LI
   LO
   TS
CP0543019
(1R,2R)-2-(4-bromo-5-fluoro-2-methylphenyl)cyclopropan-1-amine
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C10H11BrFN
 1
1
Ki = 48000 nM
   TI
   LI
   LO
   TS
CP0579349
(1R,2R)-2-(2,5-difluorophenyl)cyclopropan-1-amine
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C9H9F2N
 1
1
Ki = 53000 nM
   TI
   LI
   LO
   TS
CP0569682
(1R,2R)-2-(4-bromo-3-fluorophenyl)cyclopropan-1-amine
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C9H9BrFN
 1
1
Ki = 55000 nM
   TI
   LI
   LO
   TS
CP0577093
(1R,2R)-2-(2-fluorophenyl)cyclopropan-1-amine
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C9H10FN
 1
1
Ki = 70000 nM
   TI
   LI
   LO
   TS
CP0577534
(1R,2R)-2-(4-bromophenyl)cyclopropan-1-amine
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C9H10BrN
 1
1
Ki = 80000 nM
   TI
   LI
   LO
   TS
CP0568686
(1S,2R)-2-[2,5-difluoro-4-(3-methoxyphenyl)phenyl]cyclopropan-1-amine
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C16H15F2NO
 1
1
Ki = 86000 nM
   TI
   LI
   LO
   TS
CP0574477
5-[(1R,2R)-2-aminocyclopropyl]-2-bromophenol
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C9H10BrNO
 1
1
Ki = 88000 nM
   TI
   LI
   LO
   TS
CP0574530
(1S,2R)-2-(4-bromo-2,3-difluorophenyl)cyclopropan-1-amine
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C9H8BrF2N
 1
1
Ki = 99000 nM
   TI
   LI
   LO
   TS
CP0543018
(1S,2R)-2-(4-bromo-2-chloro-5-fluorophenyl)cyclopropan-1-amine
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C9H8BrClFN
 1
1
Ki = 100000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Lysine-specific histone demethylase 1B (KDM1B) )
Target Type Patented-recorded Target