General Information of the Protein
Protein ID
PT03383
Protein Name
Lysine-specific demethylase 6B
Secondarily
Protein Name
JmjC domain-containing protein 3
Jumonji domain-containing protein 3
Lysine demethylase 6B
[histone H3]-trimethyl-L-lysine(27) demethylase 6B
Gene Name
KDM6B
Secondarily
Gene Name
JMJD3
KIAA0346
Sequence
MHRAVDPPGARAAREAFALGGLSCAGAWSSCPPHPPPRSAWLPGGRCSASIGQPPLPAPLPPSHGSSSGHPSKPYYAPGAPTPRPLHGKLESLHGCVQALLREPAQPGLWEQLGQLYESEHDSEEATRCYHSALRYGGSFAELGPRIGRLQQAQLWNFHTGSCQHRAKVLPPLEQVWNLLHLEHKRNYGAKRGGPPVKRAAEPPVVQPVPPAALSGPSGEEGLSPGGKRRRGCNSEQTGLPPGLPLPPPPLPPPPPPPPPPPPPLPGLATSPPFQLTKPGLWSTLHGDAWGPERKGSAPPERQEQRHSLPHPYPYPAPAYTAHPPGHRLVPAAPPGPGPRPPGAESHGCLPATRPPGSDLRESRVQRSRMDSSVSPAATTACVPYAPSRPPGLPGTTTSSSSSSSSNTGLRGVEPNPGIPGADHYQTPALEVSHHGRLGPSAHSSRKPFLGAPAATPHLSLPPGPSSPPPPPCPRLLRPPPPPAWLKGPACRAAREDGEILEELFFGTEGPPRPAPPPLPHREGFLGPPASRFSVGTQDSHTPPTPPTPTTSSSNSNSGSHSSSPAGPVSFPPPPYLARSIDPLPRPPSPAQNPQDPPLVPLTLALPPAPPSSCHQNTSGSFRRPESPRPRVSFPKTPEVGPGPPPGPLSKAPQPVPPGVGELPARGPRLFDFPPTPLEDQFEEPAEFKILPDGLANIMKMLDESIRKEEEQQQHEAGVAPQPPLKEPFASLQSPFPTDTAPTTTAPAVAVTTTTTTTTTTTATQEEEKKPPPALPPPPPLAKFPPPSQPQPPPPPPPSPASLLKSLASVLEGQKYCYRGTGAAVSTRPGPLPTTQYSPGPPSGATALPPTSAAPSAQGSPQPSASSSSQFSTSGGPWARERRAGEEPVPGPMTPTQPPPPLSLPPARSESEVLEEISRACETLVERVGRSATDPADPVDTAEPADSGTERLLPPAQAKEEAGGVAAVSGSCKRRQKEHQKEHRRHRRACKDSVGRRPREGRAKAKAKVPKEKSRRVLGNLDLQSEEIQGREKSRPDLGGASKAKPPTAPAPPSAPAPSAQPTPPSASVPGKKAREEAPGPPGVSRADMLKLRSLSEGPPKELKIRLIKVESGDKETFIASEVEERRLRMADLTISHCAADVVRASRNAKVKGKFRESYLSPAQSVKPKINTEEKLPREKLNPPTPSIYLESKRDAFSPVLLQFCTDPRNPITVIRGLAGSLRLNLGLFSTKTLVEASGEHTVEVRTQVQQPSDENWDLTGTRQIWPCESSRSHTTIAKYAQYQASSFQESLQEEKESEDEESEEPDSTTGTPPSSAPDPKNHHIIKFGTNIDLSDAKRWKPQLQELLKLPAFMRVTSTGNMLSHVGHTILGMNTVQLYMKVPGSRTPGHQENNNFCSVNINIGPGDCEWFAVHEHYWETISAFCDRHGVDYLTGSWWPILDDLYASNIPVYRFVQRPGDLVWINAGTVHWVQATGWCNNIAWNVGPLTAYQYQLALERYEWNEVKNVKSIVPMIHVSWNVARTVKISDPDLFKMIKFCLLQSMKHCQVQRESLVRAGKKIAYQGRVKDEPAYYCNECDVEVFNILFVTSENGSRNTYLVHCEGCARRRSAGLQGVVVLEQYRTEELAQAYDAFTLAPASTSR
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Organism
Homo sapiens, Human
Protein Classification
Epigenetic regulator
>
Eraser
>
Lysine demethylase
>
Jumonji domain-containing
Function
Histone demethylase that specifically demethylates 'Lys-27' of histone H3, thereby playing a central role in histone code (PubMed:17825402, PubMed:17851529, PubMed:17713478, PubMed:18003914). Demethylates trimethylated and dimethylated H3 'Lys-27' (PubMed:17825402, PubMed:17851529, PubMed:17713478, PubMed:18003914). Plays a central role in regulation of posterior development, by regulating HOX gene expression (PubMed:17851529). Involved in inflammatory response by participating in macrophage differentiation in case of inflammation by regulating gene expression and macrophage differentiation (PubMed:17825402). Plays a demethylase-independent role in chromatin remodeling to regulate T-box family member-dependent gene expression by acting as a link between T-box factors and the SMARCA4-containing SWI/SNF remodeling complex (By similarity).
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Uniprot ID
Primary ID:
O15054

Secondarily ID:
C9IZ40
Q96G33
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Ensembl ID
ENSG00000132510
HGNC ID
HGNC:29012
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0412030
2-{1-[2-(3-fluorophenyl)ethyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C19H14F4N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0536543
2-{1-[2-(4-fluorophenyl)ethyl]-1H-imidazol- 4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3- triazol-4-yl]pyridine
   Show/Hide
C19H14F4N6
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0393547
2-{1-[(2-chlorophenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C18H12ClF3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393549
4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]-2-{1-[2- (2,4,5-trifluorophenyl)ethyl]-1H-imidazol-4- yl}pyridine
   Show/Hide
C19H12F6N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393550
2-{1-[2-(2-ethoxyphenyl)ethyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C21H19F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393551
2-{1-[(4-chlorophenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C18H12ClF3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393552
2-{1-[(4-methylphenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C19H15F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393553
2-{1-[2-(2-chloro-6-fluorophenyl)ethyl]-1H- imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3- triazol-4-yl]pyridine
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C19H13ClF4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393554
4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]-2- {1-[2-(2,4,6-trifluorophenyl)ethyl]-1H-imidazol- 4-yl}pyridine
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C19H12F6N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0393556
2-{1-[2-(4-tert-butylphenyl)ethyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
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C23H23F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0401730
2-{1-[2-(2,5-difluorophenyl)ethyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
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C19H13F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0401731
4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]-2-(1-{2- [4-(trifluoromethyl)phenyl]ethyl}-1H-imidazol-4- yl)pyridine
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C20H14F6N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0401741
2-[5-(4-fluorophenyl)-1-methyl-1H-imidazol-4-yl]-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C18H12F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412028
2-{1-[(4-fluorophenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C18H12F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412029
2-{1-[(4-fluoro-2-methylphenyl)methyl]-1H- imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3- triazol-4-yl]pyridine
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C19H14F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0412031
2-{1-[2-(2,3-difluorophenyl)ethyl]-1H-imidazol- 4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol- 4-yl]pyridine
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C19H13F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450661
2-{1-[2-(4-methoxyphenyl)ethyl]-1H-imidazol-4-yl}- 4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C20H17F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450667
2-{1-[(2,6-difluorophenyl)methyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
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C18H11F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450668
2-{1-[2-(4-ethylphenyl)ethyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C21H19F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450669
2-{1-[(2-methylphenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C19H15F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450670
2-(1-{[2-(2,2,2- trifluoroethoxy)phenyl]methyl}-1H- imidazol-4-yl)-4-[5-(trifluoromethyl)-1H- 1,2,3-triazol-4-yl]pyridine
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C20H14F6N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0450672
2-{1-[2-(2,4-difluorophenyl)ethyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
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C19H13F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0458071
2-{1-[(2,4-difluorophenyl)methyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
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C18H11F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0458224
2-(1-benzyl-1H-imidazol-4-yl)-4-[5- (trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C18H13F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0466684
2-{1-[2-(2,6-difluorophenyl)ethyl]-1H-imidazol-4- yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4- yl]pyridine
   Show/Hide
C19H13F5N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0536542
2-{1-[2-(2-chlorophenyl)ethyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C19H14ClF3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0540895
2-{1-[(2-fluoro-4-methylphenyl)methyl]-1H- imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3- triazol-4-yl]pyridine
   Show/Hide
C19H14F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0540901
2-{1-[(4-fluorophenyl)methyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C18H12F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0541046
2-{1-[2-(4-methylphenyl)ethyl]-1H-imidazol-4-yl}- 4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C20H17F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0547268
2-{1-[(4-methoxyphenyl)methyl]-1H-imidazol-4-yl}- 4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C19H15F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0553617
2-{1-[2-(4-chlorophenyl)ethyl]-1H-imidazol-4-yl}-4- [5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C19H14ClF3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854651
2-{1-[(5-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C22H18F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854652
2-{1-[(7-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)methy1]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C22H18F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854654
2-[1-(1-phenylpropyl)-1H-imidazol-4-yl]-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C20H17F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854655
2-{1-[(3S)-1-benzoylpiperidin-3-yl]-1H-imidazol-4-yl}-4-[5-(trifiuoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C23H20F3N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854656
2-{1-[(7-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)methy1]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridiiie
   Show/Hide
C23H21F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0854657
2-{1-[(6-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C23H21F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0859545
2-{1-[(3,4-dihydro-2H-1-benzopyranyl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C21H17F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0859567
2-{1-[(6-fluoro-1,2,3,4-tetrahydronaphthalen-1-yl)methy1]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C22H18F4N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0887459
2-{1-[(1,2,3,4,4a,8a-hexahydronaphthalen-3-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-y1]pyridine
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C22H19F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0887460
2-[1-(1-phenylethyl)-1H-imidazol-4-yl]-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C19H15F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0902854
2-[1-(2-methyl-1-phenylpropyl)-1H-imidazol-4-yl]-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C21H19F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0905310
2-{1-[(8-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C23H21F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0945746
2-{1-[(6-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C23H21F3N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0948435
2-{1-[(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methyl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C23H21F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0948441
2-{1-[(3R)-1-benzoylpiperidin-3-yl]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
   Show/Hide
C23H20F3N7O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0948482
2-{1-[(7-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)methy1]-1H-imidazol-4-yl}-4-[5-(trifluoromethyl)-1H-1,2,3-triazol-4-yl]pyridine
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C23H21F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0164116
CPI-455
   Show/Hide
C16H14N4O
 1
1
IC50 = 14300 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
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0085459
3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid
   Show/Hide
C22H23N5O2
 2
1 IC50 = 63.1 nM
2 IC50 = 150 nM
Clinical Information about the Protein
Target 1 ( Lysine-specific demethylase 6B (KDM6B) )
Target Type Literature-reported Target