General Information of the Protein
Protein ID
PT02548
Protein Name
Histone lysine demethylase PHF8
Secondarily
Protein Name
PHD finger protein 8
[histone H3]-dimethyl-L-lysine(36) demethylase PHF8
[histone H3]-dimethyl-L-lysine(9) demethylase PHF8
Gene Name
PHF8
Secondarily
Gene Name
KIAA1111
ZNF422
Sequence
MNRSRAIVQRGRVLPPPAPLDTTNLAGRRTLQGRAKMASVPVYCLCRLPYDVTRFMIECDMCQDWFHGSCVGVEEEKAADIDLYHCPNCEVLHGPSIMKKRRGSSKGHDTHKGKPVKTGSPTFVRELRSRTFDSSDEVILKPTGNQLTVEFLEENSFSVPILVLKKDGLGMTLPSPSFTVRDVEHYVGSDKEIDVIDVTRQADCKMKLGDFVKYYYSGKREKVLNVISLEFSDTRLSNLVETPKIVRKLSWVENLWPEECVFERPNVQKYCLMSVRDSYTDFHIDFGGTSVWYHVLKGEKIFYLIRPTNANLTLFECWSSSSNQNEMFFGDQVDKCYKCSVKQGQTLFIPTGWIHAVLTPVDCLAFGGNFLHSLNIEMQLKAYEIEKRLSTADLFRFPNFETICWYVGKHILDIFRGLRENRRHPASYLVHGGKALNLAFRAWTRKEALPDHEDEIPETVRTVQLIKDLAREIRLVEDIFQQNVGKTSNIFGLQRIFPAGSIPLTRPAHSTSVSMSRLSLPSKNGSKKKGLKPKELFKKAERKGKESSALGPAGQLSYNLMDTYSHQALKTGSFQKAKFNITGACLNDSDDDSPDLDLDGNESPLALLMSNGSTKRVKSLSKSRRTKIAKKVDKARLMAEQVMEDEFDLDSDDELQIDERLGKEKATLIIRPKFPRKLPRAKPCSDPNRVREPGEVEFDIEEDYTTDEDMVEGVEGKLGNGSGAGGILDLLKASRQVGGPDYAALTEAPASPSTQEAIQGMLCMANLQSSSSSPATSSLQAWWTGGQDRSSGSSSSGLGTVSNSPASQRTPGKRPIKRPAYWRTESEEEEENASLDEQDSLGACFKDAEYIYPSLESDDDDPALKSRPKKKKNSDDAPWSPKARVTPTLPKQDRPVREGTRVASIETGLAAAAAKLAQQELQKAQKKKYIKKKPLLKEVEQPRPQDSNLSLTVPAPTVAATPQLVTSSSPLPPPEPKQEALSGSLADHEYTARPNAFGMAQANRSTTPMAPGVFLTQRRPSVGSQSNQAGQGKRPKKGLATAKQRLGRILKIHRNGKLLL
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Reader
>
Plant homeodomain
Function
Histone lysine demethylase with selectivity for the di- and monomethyl states that plays a key role cell cycle progression, rDNA transcription and brain development. Demethylates mono- and dimethylated histone H3 'Lys-9' residue (H3K9Me1 and H3K9Me2), dimethylated H3 'Lys-27' (H3K27Me2) and monomethylated histone H4 'Lys-20' residue (H4K20Me1). Acts as a transcription activator as H3K9Me1, H3K9Me2, H3K27Me2 and H4K20Me1 are epigenetic repressive marks. Involved in cell cycle progression by being required to control G1-S transition. Acts as a coactivator of rDNA transcription, by activating polymerase I (pol I) mediated transcription of rRNA genes. Required for brain development, probably by regulating expression of neuron-specific genes. Only has activity toward H4K20Me1 when nucleosome is used as a substrate and when not histone octamer is used as substrate. May also have weak activity toward dimethylated H3 'Lys-36' (H3K36Me2), however, the relevance of this result remains unsure in vivo. Specifically binds trimethylated 'Lys-4' of histone H3 (H3K4me3), affecting histone demethylase specificity: has weak activity toward H3K9Me2 in absence of H3K4me3, while it has high activity toward H3K9me2 when binding H3K4me3. Positively modulates transcription of histone demethylase KDM5C, acting synergistically with transcription factor ARX; synergy may be related to enrichment of histone H3K4me3 in regulatory elements.
    Show/Hide
Uniprot ID
Primary ID:
Q9UPP1

Secondarily ID:
B3KMV4
B7Z911
Q5H9U5
Q5JPR9
Q5JPS0
Q5JPS2
Q5JPS3
Q5VUJ4
Q7Z6D4
Q9HAH2
    Show/Hide
Ensembl ID
ENSG00000172943
HGNC ID
HGNC:20672
Subcellular Location
Nucleus
Nucleus
Nucleolus
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
CP0401732
2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C17H12Cl2N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0401735
2-[1-[2-(2-chlorophenyl)-2-methylpropyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C20H19ClN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0411559
2-[1-[2-(2-chlorophenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H15ClN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0411560
2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]-4-(5-iodo-1H-triazol-4-yl)pyridine
   Show/Hide
C17H11Cl2IN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0411561
4-(5-fluoro-1H-triazol-4-yl)-2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]pyridine
   Show/Hide
C22H17FN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0412685
2-[5-(4-fluorophenyl)-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C17H13FN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0450662
2-[1-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H12ClF3N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0458068
2-[1-[2-(2-ethoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C20H20N6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0458221
2-[1-[(3-chloro-2-fluorophenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C17H12ClFN6
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0458222
1-benzyl-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H12N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0466685
2-[1-[2-(2-methoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C19H18N6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0471451
2-[1-[(2-chlorophenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C17H13ClN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0471537
2-(1-methylimidazol-4-yl)-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C11H10N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0471546
2-[1-[(2-fluoro-3-methoxyphenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H15FN6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0485473
2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C22H18N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0490859
2-[1-[(2-fluoro-3-methylphenyl)methyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridin
   Show/Hide
C18H15FN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0519463
2-[1-[2-[2-(cyclopropylmethoxy)phenyl]ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C22H22N6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0519464
4-[2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]pyridin-4-yl]-1H-triazole-5-carbonitrile
   Show/Hide
C23H17N7
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0519465
4-(1H-triazol-4-yl)-2-[1-[2-[2-(trifluoromethyl)phenyl]ethyl]imidazol-4-yl]pyridine
   Show/Hide
C19H15F3N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0540899
2-[5-(4-fluoro-3-methoxyphenyl)-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H15FN6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0548472
4-(1H-triazol-4-yl)-2-[1-[2-[2-(trifluoromethoxy)phenyl]ethyl]imidazol-4-yl]pyridine
   Show/Hide
C19H15F3N6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0551923
2-(5-bromo-1-(2-chlorobenzyl)-1H-imidazol-4-yl)-4-(2H-1,2,3-triazol-4-yl)pyridine
   Show/Hide
C17H12BrClN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0558604
4-(1H-triazol-4-yl)-2-[1-[2-[2-(2,2,2-trifluoroethoxy)phenyl]ethyl]imidazol-4-yl]pyridine
   Show/Hide
C20H17F3N6O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0561877
2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]-4-(5-fluoro-1H-triazol-4-yl)pyridine
   Show/Hide
C17H11Cl2FN6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0859546
2-[1-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C21H20N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0864774
2-[1-(3,4-dihydro-2H-chromen-4-ylmethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C20H18N6O
 1
1
IC50 <= 100 nM
   TI
   LI
   LO
   TS
CP0948434
2-[1-(1-phenylethyl)imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H16N6
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0953302
4-[2-[1-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)imidazol-4-yl]pyridin-4-yl]-1H-triazole-5-carbonitrile
   Show/Hide
C22H19N7
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0401733
2-[5-(3-ethoxy-4-fluorophenyl)-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C19H17FN6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0401737
2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]-4-(5-fluoro-1H-triazol-4-yl)pyridine
   Show/Hide
C21H18F2N6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0401738
1-[(3,4-dichlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H10Cl2N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0401739
1-(3-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C14H9ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0411562
1-[(2-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H11ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0450663
4-(5-chloro-1H-triazol-4-yl)-2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]pyridine
   Show/Hide
C22H17ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0450665
1-[(4-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H11ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0450666
1-(2-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C14H9ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0458220
2-[1-[2-(2-phenylmethoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C25H22N6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0458223
1-(3,5-dichlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C14H8Cl2N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0471536
1-[(3-chlorophenyl)methyl]-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H11ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0471547
4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1-(2,2,2-trifluoroethyl)-1H-imidazole
   Show/Hide
C10H7F3N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0471548
5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methyl-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C19H17FN6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0478994
2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C21H19FN6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0481779
1-(4-chlorophenyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C14H9ClN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0517752
1-(cyclopropylmethyl)-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C12H12N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0530608
2-[1-[2-(2-phenylphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C24H20N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0530610
5-(4-fluorophenyl)-1-methyl-4-{1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl}-1H-imidazole
   Show/Hide
C15H11FN6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0547357
4-[2-[5-2-cyclopropylmethoxy)-4- fluorophenyl]-1-methylimidazol-4- yl]pyridin-4-yl]-1H-triazole-5-carbonitrile
   Show/Hide
C22H18FN7O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0548471
2-[1-[2-(2-phenoxyphenyl)ethyl]imidazol-4-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C24H20N6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0551922
2-[1-[[2-fluoro-3-(trifluoromethoxy)phenyl]methyl]imidazol-44-yl]-4-(1H-triazol-4-yl)pyridine
   Show/Hide
C18H12F4N6O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0893597
4-[2-[1-[(2,3-dichlorophenyl)methyl]imidazol-4-yl]pyridin-4-y]]-1H-triazole-5-carbonitrile
   Show/Hide
C19H13Cl2N7
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0913811
2-(1-(1-phenylpropan-2-yl)-1H-imidazol-4-yl)-4-(1H-1,2,3-triazol-4-yl)pyridine
   Show/Hide
C19H18N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0953301
4-[2-[1-[(2-chlorophenyl)methyl]imidazol-4-yl]pyridin-4-yl]-1H-triazole-5-carbonitrile
   Show/Hide
C19H14ClN7
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0401736
4-(5-chloro-1H-triazol-4-yl)-2-[5-[2-(cyclopropylmethoxy)-4-fluorophenyl]-1-methylimidazol-4-yl]pyridine
   Show/Hide
C21H18ClFN6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450664
4-(5-iodo-1H-triazol-4-yl)-2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]pyridine
   Show/Hide
C22H17IN6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0490862
2-[1-(2-naphthalen-1-ylethyl)imidazol-4-yl]-4-[5-(trifluoromethyl)-1H-triazol-4-yl]pyridine
   Show/Hide
C23H17F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0396098
US10022354, Example 29
   Show/Hide
C15H22N4O2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0410701
US10022354, Example 78
   Show/Hide
C21H26N6O
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0420753
CHEMBL4542928
   Show/Hide
C25H33N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0424289
5-[4-[[hexyl(methyl)amino]methyl]phenyl]-7-oxo-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
   Show/Hide
C24H31N5O
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Histone lysine demethylase PHF8 (PHF8) )
Target Type Literature-reported Target