General Information of the Protein
Protein ID
PT03382
Protein Name
Lysine-specific demethylase 5B
Secondarily
Protein Name
Cancer/testis antigen 31
Histone demethylase JARID1B
Jumonji/ARID domain-containing protein 1B
PLU-1
Retinoblastoma-binding protein 2 homolog 1
[histone H3]-trimethyl-L-lysine(4) demethylase 5B
Gene Name
KDM5B
Secondarily
Gene Name
JARID1B
PLU1
RBBP2H1
Sequence
MEAATTLHPGPRPALPLGGPGPLGEFLPPPECPVFEPSWEEFADPFAFIHKIRPIAEQTGICKVRPPPDWQPPFACDVDKLHFTPRIQRLNELEAQTRVKLNFLDQIAKYWELQGSTLKIPHVERKILDLFQLNKLVAEEGGFAVVCKDRKWTKIATKMGFAPGKAVGSHIRGHYERILNPYNLFLSGDSLRCLQKPNLTTDTKDKEYKPHDIPQRQSVQPSETCPPARRAKRMRAEAMNIKIEPEETTEARTHNLRRRMGCPTPKCENEKEMKSSIKQEPIERKDYIVENEKEKPKSRSKKATNAVDLYVCLLCGSGNDEDRLLLCDGCDDSYHTFCLIPPLHDVPKGDWRCPKCLAQECSKPQEAFGFEQAARDYTLRTFGEMADAFKSDYFNMPVHMVPTELVEKEFWRLVSTIEEDVTVEYGADIASKEFGSGFPVRDGKIKLSPEEEEYLDSGWNLNNMPVMEQSVLAHITADICGMKLPWLYVGMCFSSFCWHIEDHWSYSINYLHWGEPKTWYGVPGYAAEQLENVMKKLAPELFVSQPDLLHQLVTIMNPNTLMTHEVPVYRTNQCAGEFVITFPRAYHSGFNQGFNFAEAVNFCTVDWLPLGRQCVEHYRLLHRYCVFSHDEMICKMASKADVLDVVVASTVQKDMAIMIEDEKALRETVRKLGVIDSERMDFELLPDDERQCVKCKTTCFMSAISCSCKPGLLVCLHHVKELCSCPPYKYKLRYRYTLDDLYPMMNALKLRAESYNEWALNVNEALEAKINKKKSLVSFKALIEESEMKKFPDNDLLRHLRLVTQDAEKCASVAQQLLNGKRQTRYRSGGGKSQNQLTVNELRQFVTQLYALPCVLSQTPLLKDLLNRVEDFQQHSQKLLSEETPSAAELQDLLDVSFEFDVELPQLAEMRIRLEQARWLEEVQQACLDPSSLTLDDMRRLIDLGVGLAPYSAVEKAMARLQELLTVSEHWDDKAKSLLKARPRHSLNSLATAVKEIEEIPAYLPNGAALKDSVQRARDWLQDVEGLQAGGRVPVLDTLIELVTRGRSIPVHLNSLPRLETLVAEVQAWKECAVNTFLTENSPYSLLEVLCPRCDIGLLGLKRKQRKLKEPLPNGKKKSTKLESLSDLERALTESKETASAMATLGEARLREMEALQSLRLANEGKLLSPLQDVDIKICLCQKAPAAPMIQCELCRDAFHTSCVAVPSISQGLRIWLCPHCRRSEKPPLEKILPLLASLQRIRVRLPEGDALRYMIERTVNWQHRAQQLLSSGNLKFVQDRVGSGLLYSRWQASAGQVSDTNKVSQPPGTTSFSLPDDWDNRTSYLHSPFSTGRSCIPLHGVSPEVNELLMEAQLLQVSLPEIQELYQTLLAKPSPAQQTDRSSPVRPSSEKNDCCRGKRDGINSLERKLKRRLEREGLSSERWERVKKMRTPKKKKIKLSHPKDMNNFKLERERSYELVRSAETHSLPSDTSYSEQEDSEDEDAICPAVSCLQPEGDEVDWVQCDGSCNQWFHQVCVGVSPEMAEKEDYICVRCTVKDAPSRK
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Eraser
>
Lysine demethylase
>
Jumonji domain-containing
Function
Histone demethylase that demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code (PubMed:24952722, PubMed:27214403, PubMed:28262558). Does not demethylate histone H3 'Lys-9' or H3 'Lys-27'. Demethylates trimethylated, dimethylated and monomethylated H3 'Lys-4'. Acts as a transcriptional corepressor for FOXG1B and PAX9. Favors the proliferation of breast cancer cells by repressing tumor suppressor genes such as BRCA1 and HOXA5 (PubMed:24952722). In contrast, may act as a tumor suppressor for melanoma. Represses the CLOCK-BMAL1 heterodimer-mediated transcriptional activation of the core clock component PER2 (By similarity).
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Uniprot ID
Primary ID:
Q9UGL1

Secondarily ID:
O95811
Q15752
Q9Y3Q5
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Ensembl ID
ENSG00000117139
HGNC ID
HGNC:18039
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
CP0138214
 Compound Info 
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 = 3770 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0138240
 Compound Info 
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 = 13400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0236794
 Compound Info 
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 = 20800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0061173
 Compound Info 
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 = 24200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0236796
 Compound Info 
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 = 26000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0138238
 Compound Info 
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 = 26400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0315103
 Compound Info 
2-[5-[(4- cyanophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C17H12N4O3
  1
1 IC50 = 0.6 nM
CP0068191
 Compound Info 
2-[5-[(4-chloro-2- methoxyphenyl)methoxy]pyrazol- 1-yl]pyridine-4-carboxylic acid
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C17H14ClN3O4
  1
1 IC50 = 1 nM
CP0081050
 Compound Info 
2-(4-[2-(dimethylamino)ethyl]- 5-[(4- fluorophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C20H21FN4O3
  1
1 IC50 = 1 nM
CP0081054
 Compound Info 
2-(5-(benzyloxy)-1H-pyrazol-1- yl)isonicotinic acid
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C16H13N3O3
  1
1 IC50 = 1 nM
CP0080566
 Compound Info 
2-(5-((4-chloro-2-methylbenzyl)oxy)-1Hpyrazol-1-yl)isonicotinic acid (N19)
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C17H14ClN3O3
  1
1 IC50 = 2 nM
CP0081048
 Compound Info 
2-{5-[(4-bromobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12BrN3O3
  1
1 IC50 = 2 nM
CP0111516
 Compound Info 
2-{5-[(4-ethylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridine- 4-carboxylic acid
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C18H17N3O3
  1
1 IC50 = 3 nM
CP0164116
 Compound Info 
CPI-455
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C16H14N4O
  2
1 IC50 = 3 nM
2 IC50 = 10 nM
CP0068188
 Compound Info 
2-{5-[(4-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
  1
1 IC50 = 4 nM
CP0080564
 Compound Info 
2-{5-[(4-chloro-2- fluorobenzyl)oxy]-1H-pyrazol-1- yl}pyridine-4-carboxylic acid
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C16H11ClFN3O3
  1
1 IC50 = 4 nM
CP0080567
 Compound Info 
2-{5-[(4-methylbenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C17H15N3O3
  1
1 IC50 = 4 nM
CP0081057
 Compound Info 
2-[5-[(4-chloro-2- ethoxyphenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C18H16ClN3O4
  1
1 IC50 = 4 nM
CP0120868
 Compound Info 
2-[5-[(4-chlorophenyl)methoxy]pyrazol-1-yl]pyridine-4-carboxylic acid
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C16H12ClN3O3
  1
1 IC50 = 4 nM
CP0120871
 Compound Info 
2-[5-[(4-chloro-2- phenylmethoxyphenyl)methoxy] pyrazol-1-yl]pyridine-4-carboxylic acid
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C23H18ClN3O4
  1
1 IC50 = 4 nM
CP0239479
 Compound Info 
2-{5-[(4-methoxybenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C17H15N3O4
  1
1 IC50 = 4 nM
CP0134733
 Compound Info 
CHEMBL3785583
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C17H20N6O
  1
1 IC50 = 4.7 nM
CP0138240
 Compound Info 
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
  13
1 IC50 = 5 nM
2 IC50 = 7 nM
3 IC50 = 9 nM
4 IC50 = 11 nM
5 IC50 = 16 nM
6 IC50 = 23 nM
7 IC50 = 38 nM
8 IC50 = 39 nM
9 IC50 = 104 nM
10 IC50 = 177 nM
11 IC50 = 371 nM
12 IC50 = 947 nM
13 Ki = 7 nM
CP0248901
 Compound Info 
2-[5-[[4-chloro-2- (cyclopropylmethoxy(phenyl] methoxy]pyrazol-1-yl]pyridine- 4-carboxylic acid
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C20H18ClN3O4
  1
1 IC50 = 6 nM
CP0138214
 Compound Info 
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
  2
1 IC50 = 6 nM
2 Ki = 1 nM
CP0239480
 Compound Info 
2-{5-[(4-cyclopropylbenzyl)oxy]- 1H-pyrazol-1-yl}pyridine-4- carboxylic acid
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C19H17N3O3
  1
1 IC50 = 8 nM
CP0234557
 Compound Info 
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
  2
1 IC50 = 12 nM
2 Ki = 4 nM
CP0236794
 Compound Info 
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
  2
1 IC50 = 14 nM
2 Ki = 2 nM
CP0236796
 Compound Info 
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
  2
1 IC50 = 17 nM
2 Ki = 1 nM
CP0392139
 Compound Info 
2-{5-[(3-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
  1
1 IC50 = 22 nM
CP0061173
 Compound Info 
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
  2
1 IC50 = 23 nM
2 Ki = 2 nM
CP0080562
 Compound Info 
2-[4-ethyl-5-[(4- fluorophenyl)methoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C18H16FN3O3
  1
1 IC50 = 24 nM
CP0138235
 Compound Info 
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
  2
1 IC50 = 29 nM
2 Ki = 3 nM
CP0068190
 Compound Info 
2-[5-[1-(4- fluorophenyl)ethoxy]pyrazol-1- yl]pyridine-4-carboxylic acid
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C17H14FN3O3
  1
1 IC50 = 41 nM
CP0080560
 Compound Info 
2-{5-[(2-fluorobenzyl)oxy]-1H- pyrazol-1-yl}pyridine-4- carboxylic acid
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C16H12FN3O3
  1
1 IC50 = 42 nM
CP0329706
 Compound Info 
2-[5-[(4-fluorophenyl)methoxy]-4- methylpyrazol-1-yl]pyridine-4- carboxylic acid
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C17H14FN3O3
  1
1 IC50 = 54 nM
CP0396098
 Compound Info 
US10022354, Example 29
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C15H22N4O2
  1
1 IC50 = 60 nM
CP0239481
 Compound Info 
2-[5-[(4-fluorophenyl)methoxy]-4-(2-hydroxyethyl)pyrazol-1-yl]pyridine-4-carboxylic acid
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C18H16FN3O4
  1
1 IC50 = 68 nM
CP0081052
 Compound Info 
2-(5-(3-hydroxy-4-methylphenyl)- 1H-pyrazol-1-yl)isonicotinic acid
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C16H13N3O3
  1
1 IC50 = 76 nM
CP0111518
 Compound Info 
2-(5-(3-hydroxyphenyl)-1H- pyrazol-1-yl)isonicotinic acid
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C15H11N3O3
  1
1 IC50 = 120 nM
CP0138238
 Compound Info 
8-[4-[1-(cyclobutylmethyl)piperidin-4-yl]pyrazol-1-yl]-3H-pyrido[3,4-d]pyrimidin-4-one
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C20H24N6O
  2
1 IC50 = 134 nM
2 Ki = 16 nM
CP0536157
 Compound Info 
2-(5-(2,4-difluorophenyl)-1H- pyrazol-1-yl)isonicotinic acid
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C15H9F2N3O2
  1
1 IC50 = 170 nM
CP0237641
 Compound Info 
2-(5-p-tolyl-1H-pyrazol-1- yl)isonicotinic acid
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C16H13N3O2
  1
1 IC50 = 200 nM
CP0530567
 Compound Info 
2-(5-(4-chloro-3-methoxyphenyl)- 1H-pyrazol-1-yl)isonicotinic acid
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C16H12ClN3O3
  1
1 IC50 = 230 nM
CP0248899
 Compound Info 
2-(5-(4-fluorophenyl)-1H-pyrazol- 1-yl)isonicotinic acid
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C15H10FN3O2
  1
1 IC50 = 240 nM
CP0237640
 Compound Info 
2-(5-(4-hydroxyphenyl)-1H- pyrazol-1-yl)isonicotinic acid
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C15H11N3O3
  1
1 IC50 = 320 nM
CP0080570
 Compound Info 
2-(5-(4-(methylsulfonyl)phenyl)- 1H-pyrazol-1-yl)isonicotinic acid
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C16H13N3O4S
  1
1 IC50 = 350 nM
CP0081047
 Compound Info 
2-(5-(3,4-difluorophenyl)-1H- pyrazol-1-yl)isonicotinic acid
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C15H9F2N3O2
  1
1 IC50 = 370 nM
CP0364520
 Compound Info 
2-(5-(3-fluorophenyl)-1H-pyrazol- 1-yl)isonicotinic acid
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C15H10FN3O2
  1
1 IC50 = 500 nM
CP0239483
 Compound Info 
2-(5-(3-methoxy-4-methylphenyl)- 1H-pyrazol-1-yl)isonicotinic acid
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C17H15N3O3
  1
1 IC50 = 540 nM
CP0215948
 Compound Info 
2-(5-phenyl-1H-pyrazol-1- yl)isonicotinic acid
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C15H11N3O2
  1
1 IC50 = 4400 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 5B (KDM5B) )
Target Type Literature-reported Target