General Information of the Protein
Protein ID
PT04390
Protein Name
Lysine-specific demethylase 4B
Secondarily
Protein Name
JmjC domain-containing histone demethylation protein 3B
Jumonji domain-containing protein 2B
[histone H3]-trimethyl-L-lysine(9) demethylase 4B
Gene Name
KDM4B
Secondarily
Gene Name
JHDM3B
JMJD2B
KIAA0876
Sequence
MGSEDHGAQNPSCKIMTFRPTMEEFKDFNKYVAYIESQGAHRAGLAKIIPPKEWKPRQTYDDIDDVVIPAPIQQVVTGQSGLFTQYNIQKKAMTVGEYRRLANSEKYCTPRHQDFDDLERKYWKNLTFVSPIYGADISGSLYDDDVAQWNIGSLRTILDMVERECGTIIEGVNTPYLYFGMWKTTFAWHTEDMDLYSINYLHFGEPKSWYAIPPEHGKRLERLAIGFFPGSSQGCDAFLRHKMTLISPIILKKYGIPFSRITQEAGEFMITFPYGYHAGFNHGFNCAESTNFATLRWIDYGKVATQCTCRKDMVKISMDVFVRILQPERYELWKQGKDLTVLDHTRPTALTSPELSSWSASRASLKAKLLRRSHRKRSQPKKPKPEDPKFPGEGTAGAALLEEAGGSVKEEAGPEVDPEEEEEEPQPLPHGREAEGAEEDGRGKLRPTKAKSERKKKSFGLLPPQLPPPPAHFPSEEALWLPSPLEPPVLGPGPAAMEESPLPAPLNVVPPEVPSEELEAKPRPIIPMLYVVPRPGKAAFNQEHVSCQQAFEHFAQKGPTWKEPVSPMELTGPEDGAASSGAGRMETKARAGEGQAPSTFSKLKMEIKKSRRHPLGRPPTRSPLSVVKQEASSDEEASPFSGEEDVSDPDALRPLLSLQWKNRAASFQAERKFNAAAARTEPYCAICTLFYPYCQALQTEKEAPIASLGKGCPATLPSKSRQKTRPLIPEMCFTSGGENTEPLPANSYIGDDGTSPLIACGKCCLQVHASCYGIRPELVNEGWTCSRCAAHAWTAECCLCNLRGGALQMTTDRRWIHVICAIAVPEARFLNVIERHPVDISAIPEQRWKLKCVYCRKRMKKVSGACIQCSYEHCSTSFHVTCAHAAGVLMEPDDWPYVVSITCLKHKSGGHAVQLLRAVSLGQVVITKNRNGLYYRCRVIGAASQTCYEVNFDDGSYSDNLYPESITSRDCVQLGPPSEGELVELRWTDGNLYKAKFISSVTSHIYQVEFEDGSQLTVKRGDIFTLEEELPKRVRSRLSLSTGAPQEPAFSGEEAKAAKRPRVGTPLATEDSGRSQDYVAFVESLLQVQGRPGAPF
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Eraser
>
Lysine demethylase
>
Lysine-specific demethylase
Function
Histone demethylase that specifically demethylates 'Lys-9' of histone H3, thereby playing a role in histone code. Does not demethylate histone H3 'Lys-4', H3 'Lys-27', H3 'Lys-36' nor H4 'Lys-20'. Only able to demethylate trimethylated H3 'Lys-9', with a weaker activity than KDM4A, KDM4C and KDM4D. Demethylation of Lys residue generates formaldehyde and succinate (PubMed:16603238, PubMed:28262558). Plays a critical role in the development of the central nervous system (CNS).
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Uniprot ID
Primary ID:
O94953

Secondarily ID:
B9EGN8
D6W631
O75274
Q6P3R5
Q9P1V1
Q9UF40
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HGNC ID
HGNC:29136
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: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0061173
8-[4-[2-[4-(3-chlorophenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C23H23ClN6O
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0138240
8-[4-(2-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylethyl)pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C25H26N6O
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0236796
8-[4-[2-[4-(3-pyridin-3-ylphenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C28H27N7O
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0236794
8-[4-[2-[4-(3-chlorophenyl)-4-methylpiperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C24H25ClN6O
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0138235
8-[4-[2-[4-(3-fluorophenyl)piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C23H23FN6O
 1
1
EC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0138214
8-[4-[2-[4-[3-[2-(dimethylamino)ethyl]phenyl]piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C27H33N7O
 1
1
EC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0234557
8-[4-[2-[4-[4-[2-(dimethylamino)ethyl]phenyl]piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C27H33N7O
 1
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0138238
8-[4-[1-(cyclobutylmethyl)piperidin-4-yl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C20H24N6O
 1
1
EC50 = 9100 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0138214
8-[4-[2-[4-[3-[2-(dimethylamino)ethyl]phenyl]piperidin-1-yl]ethyl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C27H33N7O
 11
1 IC50 = 4 nM
2 IC50 = 6 nM
3 IC50 = 8 nM
4 IC50 = 12 nM
5 IC50 = 21 nM
6 IC50 = 36 nM
7 IC50 = 62 nM
8 IC50 = 138 nM
9 IC50 = 270 nM
10 IC50 = 568 nM
11 IC50 = 1044 nM
CP0138240
8-[4-(2-spiro[1,2-dihydroindene-3,4'-piperidine]-1'-ylethyl)pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C25H26N6O
 11
1 IC50 = 5 nM
2 IC50 = 8 nM
3 IC50 = 12 nM
4 IC50 = 22 nM
5 IC50 = 36 nM
6 IC50 = 62 nM
7 IC50 = 96 nM
8 IC50 = 233 nM
9 IC50 = 382 nM
10 IC50 = 524 nM
11 IC50 = 787 nM
CP0250407
3-(8-hydroxyquinolin-6-yl)-N-(3-phenylpropyl)benzamide
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C25H22N2O2
 1
1 IC50 = 10 nM
CP0138238
8-[4-[1-(cyclobutylmethyl)piperidin-4-yl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C20H24N6O
 11
1 IC50 = 40 nM
2 IC50 = 66 nM
3 IC50 = 121 nM
4 IC50 = 265 nM
5 IC50 = 477 nM
6 IC50 = 564 nM
7 IC50 = 1106 nM
8 IC50 = 2437 nM
9 IC50 = 4209 nM
10 IC50 = 8680 nM
11 IC50 = 11060 nM