General Information of the Protein
Protein ID
PT01072
Protein Name
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
Secondarily
Protein Name
Inducible I kappa-B kinase
Gene Name
IKBKE
Secondarily
Gene Name
IKKE
IKKI
KIAA0151
Sequence
MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLRKLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVVAGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYLHPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTEKPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFAETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCVLEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLGAGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSVAGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSIQQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKYQASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKGAQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Other protein kinase group
Function
Serine/threonine kinase that plays an essential role in regulating inflammatory responses to viral infection, through the activation of the type I IFN, NF-kappa-B and STAT signaling. Also involved in TNFA and inflammatory cytokines, like Interleukin-1, signaling. Following activation of viral RNA sensors, such as RIG-I-like receptors, associates with DDX3X and phosphorylates interferon regulatory factors (IRFs), IRF3 and IRF7, as well as DDX3X. This activity allows subsequent homodimerization and nuclear translocation of the IRF3 leading to transcriptional activation of pro-inflammatory and antiviral genes including IFNB. In order to establish such an antiviral state, IKBKE forms several different complexes whose composition depends on the type of cell and cellular stimuli. Thus, several scaffolding molecules including IPS1/MAVS, TANK, AZI2/NAP1 or TBKBP1/SINTBAD can be recruited to the IKBKE-containing-complexes. Activated by polyubiquitination in response to TNFA and interleukin-1, regulates the NF-kappa-B signaling pathway through, at least, the phosphorylation of CYLD. Phosphorylates inhibitors of NF-kappa-B thus leading to the dissociation of the inhibitor/NF-kappa-B complex and ultimately the degradation of the inhibitor. In addition, is also required for the induction of a subset of ISGs which displays antiviral activity, may be through the phosphorylation of STAT1 at 'Ser-708'. Phosphorylation of STAT1 at 'Ser-708' seems also to promote the assembly and DNA binding of ISGF3 (STAT1:STAT2:IRF9) complexes compared to GAF (STAT1:STAT1) complexes, in this way regulating the balance between type I and type II IFN responses. Protects cells against DNA damage-induced cell death. Also plays an important role in energy balance regulation by sustaining a state of chronic, low-grade inflammation in obesity, wich leads to a negative impact on insulin sensitivity. Phosphorylates AKT1.
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Uniprot ID
Primary ID:
Q14164

Secondarily ID:
D3DT78
Q3B754
Q3KR43
Q5JTS6
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Ensembl ID
ENSG00000263528
HGNC ID
HGNC:14552
Subcellular Location
Cytoplasm
Nucleus
Nucleus
PML body
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
CP0390827
2-amino-7-cyclohexyl-3-(2H-tetrazol-5-yl)chromeno[2,3-b]pyridin-5-one
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C19H18N6O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0393323
2-amino-7-morpholin-4-yl-5-oxo-N-(2H-tetrazol-5-yl)chromeno[2,3-b]pyridine-3-carboxamide
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C18H16N8O4
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0415568
US10214536, Compound 78
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C21H18N2O6
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0390731
US10214536, Compound 8
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C17H14N2O4
 1
1
IC50 = 3100 nM
   TI
   LI
   LO
   TS
CP0427007
US10214536, Compound 80
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C21H20N2O6
 1
1
IC50 = 3200 nM
   TI
   LI
   LO
   TS
CP0429220
US10214536, Compound 38
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C19H17N3O5
 1
1
IC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0434898
US10214536, Compound 13
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C19H16N2O4
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
   TS
CP0387364
US10214536, Compound 11
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C18H16N2O4
 1
1
IC50 = 6300 nM
   TI
   LI
   LO
   TS
CP0457711
US10214536, Compound 5
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C16H12N2O4
 1
1
IC50 = 10600 nM
   TI
   LI
   LO
   TS
CP0415565
US10214536, Compound 76
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C18H16N2O6S
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0457712
US10214536, Compound 42
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C18H16N2O5
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0905363
4-(4-(benzyloxy)phenyl)-5-methyl-1H-pyrazol-3-amine
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C17H17N3O
 1
1
IC50 = 15400 nM
   TI
   LI
   LO
   TS
CP0876660
1-(5-amino-4-bromo-3-methyl-1H-pyrazol-1-yl)ethan-1-one
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C6H8BrN3O
 1
1
IC50 = 22900 nM
   TI
   LI
   LO
   TS
CP0880318
4-(3-chlorophenyl)-5-methyl-1H-pyrazol-3-amine
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C10H10ClN3
 1
1
IC50 = 93400 nM
   TI
   LI
   LO
   TS
CP0184914
4-[3-[2-amino-5-(2-methoxyethoxy)pyrimidin-4-yl]-1H-indol-5-yl]-2-methylbut-3-yn-2-ol
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C20H22N4O3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0357240
5-methyl-4-phenyl-1H-pyrazol-3-amine
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C10H11N3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0639989
1-(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)ethan-1-one
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C12H11Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0852538
1-(3-amino-4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-1-yl)ethan-1-one
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C12H11Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852539
4-(3,4-dichlorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine
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C11H11Cl2N3
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852540
N-(4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-3-yl)-2,2,2-trifluoroacetamide
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C12H8Cl2F3N3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852541
4-(4-bromophenyl)-5-methyl-1H-pyrazol-3-amine
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C10H10BrN3
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852542
N-(5-chloro-9H-pyrido[3,4-b]indol-7-yl)nicotinamide
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C17H11ClN4O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852543
1-(5-amino-4-(3,4-dichlorophenyl)-3-ethyl-1H-pyrazol-1-yl)ethan-1-one
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C13H13Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852545
4-(benzo[d][1,3]dioxol-5-yl)-5-methyl-1H-pyrazol-3-amine
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C11H11N3O2
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852546
5-methyl-4-p-tolyl-1H-pyrazol-3-amine
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C11H13N3
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0852547
1-(5-amino-3-methyl-4-(3-(trifluoromethyl)phenyl)-1H-pyrazol-1-yl)ethan-1-one
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C13H12F3N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0864824
1-(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)butan-1-one
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C14H15Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0864825
(5-amino-4-(4-chlorophenyl)-3-methyl-1H-pyrazol-1-yl)(cyclopropyl)methanone
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C14H14ClN3O
 1
1
IC50 > 100000 nM
   TI
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CP0864826
5-methyl-4-(naphthalen-2-yl)-1H-pyrazol-3-amine
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C14H13N3
 1
1
IC50 > 100000 nM
   TI
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CP0864827
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(cyclohexyl)methanone
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C17H19Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0864828
1-(3-amino-4-bromo-5-methyl-1H-pyrazol-1-yl)ethan-1-one
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C6H8BrN3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0864830
N-[4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-3-yl]pyridine-2-carboxamide
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C16H12Cl2N4O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0864831
1-(5-amino-4-(4-chlorophenyl)-3-methyl-1H-pyrazol-1-yl)ethan-1-one
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C12H12ClN3O
 1
1
IC50 > 100000 nM
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   LI
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CP0869606
SID24808657
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C10H10ClN3
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0876657
4-(3,4-dichlorophenyl)-1,5-dimethyl-1H-pyrazol-3-amine
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C11H11Cl2N3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0876658
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(cyclopropyl)methanone
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C14H13Cl2N3O
 1
1
IC50 > 100000 nM
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   LI
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CP0876659
5-methyl-4-(3-methylphenyl)-1H-pyrazol-3-amine
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C11H13N3
 1
1
IC50 > 100000 nM
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CP0880319
5-methyl-4-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine
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C11H10F3N3
 1
1
IC50 > 100000 nM
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CP0893469
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(cyclopentyl)methanone
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C16H17Cl2N3O
 1
1
IC50 > 100000 nM
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CP0893470
(3-amino-4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-1-yl)(cyclobutyl)methanone
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C15H15Cl2N3O
 1
1
IC50 > 100000 nM
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   LI
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CP0893471
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(pyridin-4-yl)methanone
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C16H12Cl2N4O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0893477
tert-butyl 5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazole-1-carboxylate
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C15H17Cl2N3O2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0893478
5-amino-4-(3,4-dichlorophenyl)-N-ethyl-3-methyl-1H-pyrazole-1-carboxamide
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C13H14Cl2N4O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0893479
4-(3-bromophenyl)-5-methyl-1H-pyrazol-3-amine
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C10H10BrN3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0893480
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(pyridin-3-yl)methanone
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C16H12Cl2N4O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0905359
1-(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)propan-1-one
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C13H13Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0905360
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(cyclobutyl)methanone
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C15H15Cl2N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
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CP0905361
(3-amino-4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-1-yl)(pyridin-3-yl)methanone
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C16H12Cl2N4O
 1
1
IC50 > 100000 nM
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   LI
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CP0905362
5-methyl-4-(3-(trifluoromethoxy)phenyl)-1H-pyrazol-3-amine
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C11H10F3N3O
 1
1
IC50 > 100000 nM
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CP0911844
1-(5-amino-4-(3,4-dimethylphenyl)-3-methyl-1H-pyrazol-1-yl)ethan-1-one
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C14H17N3O
 1
1
IC50 > 100000 nM
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CP0911845
1-(5-amino-4-(3-chlorophenyl)-3-methyl-1H-pyrazol-1-yl)ethan-1-one
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C12H12ClN3O
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0915202
4-(3,5-bis(trifluoromethyl)phenyl)-5-methyl-1H-pyrazol-3-amine
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C12H9F6N3
 1
1
IC50 > 100000 nM
   TI
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CP0915203
(5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl)(phenyl)methanone
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C17H13Cl2N3O
 1
1
IC50 > 100000 nM
   TI
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CP0915204
4-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-3-amine
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C10H9Cl2N3
 1
1
IC50 > 100000 nM
   TI
   LI
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CP0915205
5-(3,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-amine
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C10H9Cl2N3
 1
1
IC50 > 100000 nM
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CP0945628
4-(3,4-dimethylphenyl)-5-methyl-1H-pyrazol-3-amine
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C12H15N3
 1
1
IC50 > 100000 nM
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CP0386621
US10214536, Compound 15
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C19H18N2O4
 1
1
IC50 > 100000 nM
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CP0382649
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
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C50H56BF2N7O7
 1
1
Kd = 44 nM
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CP0382724
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide
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C49H54BF2N7O7
 1
1
Kd = 58 nM
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