General Information of the Protein
Protein ID
PT01223
Protein Name
Aurora kinase B
Secondarily
Protein Name
Aurora 1
Aurora- and IPL1-like midbody-associated protein 1
Aurora/IPL1-related kinase 2
STK-1
Serine/threonine-protein kinase 12
Serine/threonine-protein kinase 5
Serine/threonine-protein kinase aurora-B
Gene Name
AURKB
Secondarily
Gene Name
AIK2
AIM1
AIRK2
ARK2
STK1
STK12
STK5
Sequence
MAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMENSSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEHQLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATIMEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYLPPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPMGAQDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Other protein kinase group
>
Other protein kinase AUR family
Function
Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis (PubMed:11516652, PubMed:12925766, PubMed:14610074, PubMed:14722118, PubMed:29449677). The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly (PubMed:11516652, PubMed:12925766, PubMed:14610074, PubMed:14722118, PubMed:26829474). Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis (PubMed:15249581). Required for central/midzone spindle assembly and cleavage furrow formation (PubMed:12458200, PubMed:12686604). Key component of the cytokinesis checkpoint, a process required to delay abscission to prevent both premature resolution of intercellular chromosome bridges and accumulation of DNA damage: phosphorylates CHMP4C, leading to retain abscission-competent VPS4 (VPS4A and/or VPS4B) at the midbody ring until abscission checkpoint signaling is terminated at late cytokinesis (PubMed:22422861, PubMed:24814515). AURKB phosphorylates the CPC complex subunits BIRC5/survivin, CDCA8/borealin and INCENP (PubMed:11516652, PubMed:12925766, PubMed:14610074). Phosphorylation of INCENP leads to increased AURKB activity (PubMed:11516652, PubMed:12925766, PubMed:14610074). Other known AURKB substrates involved in centromeric functions and mitosis are CENPA, DES/desmin, GPAF, KIF2C, NSUN2, RACGAP1, SEPTIN1, VIM/vimentin, HASPIN, and histone H3 (PubMed:11784863, PubMed:12689593, PubMed:14602875, PubMed:11856369, PubMed:16103226, PubMed:21658950, PubMed:11756469). A positive feedback loop involving HASPIN and AURKB contributes to localization of CPC to centromeres (PubMed:21658950). Phosphorylation of VIM controls vimentin filament segregation in cytokinetic process, whereas histone H3 is phosphorylated at 'Ser-10' and 'Ser-28' during mitosis (H3S10ph and H3S28ph, respectively) (PubMed:11784863, PubMed:11856369). AURKB is also required for kinetochore localization of BUB1 and SGO1 (PubMed:15020684, PubMed:17617734). Phosphorylation of p53/TP53 negatively regulates its transcriptional activity (PubMed:20959462). Key regulator of active promoters in resting B- and T-lymphocytes: acts by mediating phosphorylation of H3S28ph at active promoters in resting B-cells, inhibiting RNF2/RING1B-mediated ubiquitination of histone H2A and enhancing binding and activity of the USP16 deubiquitinase at transcribed genes (By similarity). Acts as an inhibitor of CGAS during mitosis: catalyzes phosphorylation of the N-terminus of CGAS during the G2-M transition, blocking CGAS liquid phase separation and activation, and thereby preventing CGAS-induced autoimmunity (PubMed:33542149). Phosphorylates KRT5 during anaphase and telophase (By similarity).
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Uniprot ID
Primary ID:
Q96GD4

Secondarily ID:
B4DNM4
C7G533
C7G534
C7G535
D3DTR4
J9JID1
O14630
O60446
O95083
Q96DV5
Q9UQ46
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Ensembl ID
ENSG00000178999
HGNC ID
HGNC:11390
Subcellular Location
Nucleus
Chromosome
Chromosome
Centromere
Chromosome
Centromere
Kinetochore
Cytoplasm
Cytoskeleton
Spindle
Midbody
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: CL000023 , BTI-Tn-5B1-4
Compound ID Compound Name Compound Formula
CP0477498
N-[3-[(E)-2-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]ethenyl]-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C27H29N5OS
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0376394
1-phenyl-N-(3-styryl-1H-indazol-5-yl)methanesulfonamide
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C22H19N3O2S
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0430624
3-methyl-5-(4-methyl-3-(3-((4-methylpiperazin-1-yl)methyl)styryl)-1H-indazol-5-yl)aniline
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C29H33N5
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0430625
4-methyl-N-(3-(2-(6-methyl-5-(2-(thiophen-2-yl)acetamido)-1H-indazol-3-yl)vinyl)phenyl)piperazine-1-carboxamide
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C28H30N6O2S
 1
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
CP0470476
5-(pyridin-4-yl)-6-(pyrrolidin-1-yl)-3-styryl-1H-indazole
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C24H22N4
 1
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
CP0470449
N-[6-methyl-3-[(E)-2-phenylethenyl]-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C22H19N3OS
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0417624
4-methyl-3-(3-((4-methylpiperazin-1-yl)methyl)styryl)-1H-indazole-5-carbonitrile
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C23H25N5
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0430626
4-methyl-N-(3-(2-(5-(methylsulfonamido)-6-(pyrrolidin-1-yl)-1H-indazol-3-yl)vinyl)phenyl)piperazine-1-carboxamide
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C26H33N7O3S
 1
1
IC50 = 62 nM
   TI
   LI
   LO
   TS
CP0477501
6-(pyrrolidin-1-yl)-3-styryl-1H-indazol-5-amine
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C19H20N4
 1
1
IC50 = 81 nM
   TI
   LI
   LO
   TS
CP0470045
N-[4-methyl-3-[(E)-2-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]ethenyl]-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C28H31N5OS
 1
1
IC50 = 99 nM
   TI
   LI
   LO
   TS
CP0376393
5-nitro-6-(pyrrolidin-1-yl)-3-styryl-1H-indazole
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C19H18N4O2
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0477500
N-[3-[(E)-2-phenylethenyl]-6-pyrrolidin-1-yl-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C25H24N4OS
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0502849
N-[6-methyl-3-(2-phenylethynyl)-2H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C22H17N3OS
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0376392
N-[6-methyl-3-[(E)-2-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]ethenyl]-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
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C28H31N5OS
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0494484
3-[(E)-2-phenylethenyl]-N-(pyridin-2-ylmethyl)-6-pyrrolidin-1-yl-1H-indazol-5-amine
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C25H25N5
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0452085
2-(2,5-dimethoxyphenyl)-N-(6-methyl-3-styryl-1H-indazol-5-yl)acetamide
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C26H25N3O3
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0504238
6-(4-methylpiperazin-1-yl)-N-(pyridin-2-ylmethyl)-3-styryl-1H-indazol-5-amine
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C26H28N6
 1
1
IC50 = 810 nM
   TI
   LI
   LO
   TS
CP0470451
2-phenyl-N-(3-(2-phenylcyclopropyl)-1H-indazol-5-yl)acetamide
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C24H21N3O
 1
1
IC50 = 1640 nM
   TI
   LI
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0036050
2-{3-[(7-{3-[ethyl(2-hydroxyethyl)amino]propoxy}quinazolin-4-yl)amino]-1H-pyrazol-5-yl}-N-(3-fluorophenyl)acetamide
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C26H30FN7O3
 6
1 IC50 = 0.3 nM
2 IC50 = 0.37 nM
3 IC50 < 1 nM
4 Kd = 4.6 nM
5 Kd = 7.2 nM
6 Ki < 1 nM
CP0057301
4-fluoro-N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]-2-(trifluoromethyl)benzamide
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C26H16F4N4O2
 1
1 IC50 = 0.4 nM
CP0045201
2-{3-[(7-{3-[ethyl(2-hydroxyethyl)amino]propoxy}-6-methoxyquinazolin-4-yl)amino]-1H-pyrazol-5-yl}-N-(3-fluorophenyl)acetamide
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C27H32FN7O4
 2
1 IC50 = 1 nM
2 Ki = 1 nM
CP0045203
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide
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C27H31F2N7O4
 2
1 IC50 < 1 nM
2 Ki < 1 nM
CP0058393
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(propyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide
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C28H33F2N7O4
 2
1 IC50 < 1 nM
2 Ki < 1 nM
CP0161066
N-(2,3-difluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(2-methylpropyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide
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C29H35F2N7O4
 2
1 IC50 < 1 nM
2 Ki < 1 nM
CP0057282
N-[4-[(6-oxo-5H-benzo[c][1,8]naphthyridin-1-yl)amino]phenyl]benzamide
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C25H18N4O2
 1
1 IC50 = 1 nM
CP0674596
(-)-Ethyl 8-Oxo-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-4,5,6,7,8,9-hexahydro-2H-pyrrolo[3,4-b]quinoline-3-carboxylate
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C27H24N4O4
 1
1 IC50 = 1 nM
CP0058391
N-(3-fluorophenyl)-2-[3-[[7-[3-[2-hydroxyethyl(propyl)amino]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide
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C28H34FN7O4
 2
1 IC50 = 2 nM
2 Ki = 2 nM
CP0294246
N-(3-fluorophenyl)-2-[3-[[7-[3-[4-(hydroxymethyl)piperidin-1-yl]propoxy]-6-methoxyquinazolin-4-yl]amino]-1H-pyrazol-5-yl]acetamide
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C29H34FN7O4
 1
1 IC50 = 2 nM
CP0361417
CHEMBL4563026
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C33H34ClFN7O3
 1
1 IC50 = 2.55 nM
CP0042568
3-cyclopropyl-1-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazol-4-yl}urea
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C19H23N7O2
 3
1 IC50 = 2.7 nM
2 IC50 = 3 nM
3 IC50 = 62 nM
CP0026409
2-anilino-N-[4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]benzamide
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C29H24N6O2
 1
1 IC50 = 9 nM
CP0025009
Bisanilinopyrimidine, 9m
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C17H13ClFN5O
 1
1 IC50 = 10.7 nM
CP0043422
4-[6-amino-7-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]furo[3,2-c]pyridin-3-yl]-3,6-dihydro-2H-pyridine-1-carboxamide
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C21H19Cl2FN4O3
 1
1 IC50 = 11 nM
CP0645780
2-(ethyl((5-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-ylamino)isothiazol-3-yl)methyl)amino)-2-methylpropan-1-ol Hydrochloride
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C20H27ClN8OS
 1
1 IC50 <= 13 nM
CP0647070
N-[3-[(3,3-Difluoro-1-pyrrolidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C18H19ClF2N8S
 1
1 IC50 <= 13 nM
CP0647442
6-Methyl-3-(1H-pyrazol-4-yl)-N-[3-[[(3,3,3-trifluoropropyl)-amino]methyl]-5-isothiazolyl]imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C17H18ClF3N8S
 1
1 IC50 <= 13 nM
CP0647443
N-[3-[(4-Fluoro-1-piperidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H22ClFN8S
 1
1 IC50 <= 13 nM
CP0647444
N-[3-[(3(R)-Fluoro-1-pyrrolidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C18H20ClFN8S
 1
1 IC50 <= 13 nM
CP0647445
6-Methyl-3-(1H-pyrazol-4-yl)-N-[3-[(3,3,4,4-tetrafluoro-1-pyrrolidinyl)methyl]-5-isothiazolyl]imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C18H17ClF4N8S
 1
1 IC50 <= 13 nM
CP0656034
N-[3-[(4,4-Difluoro-1-piperidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H21ClF2N8S
 1
1 IC50 <= 13 nM
CP0656035
2-[(2,2-Difluoroethyl)[[5-[[6-methyl-3-(1Hpyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-isothiazolyl]methyl]-amino]-2-methyl-1-propanol Hydrochloride
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C20H25ClF2N8OS
 1
1 IC50 <= 13 nM
CP0657138
Deuterated N-[3-[(3,3-Difluoro-1-pyrrolidinyl)methyl-(d2)]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C18H19ClF2N8S
 1
1 IC50 <= 13 nM
CP0680616
6-Methyl-N-[3-(1-piperidinylmethyl)-5-isothiazolyl]-3-(1Hpyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H23ClN8S
 1
1 IC50 <= 13 nM
CP0701989
6-Methyl-N-[3-[[(2,2,3,3,3-pentafluoropropyl)amino]methyl]-5-isothiazolyl]-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C17H16ClF5N8S
 1
1 IC50 <= 13 nM
CP0702733
6-Methyl-3-(1H-pyrazol-4-yl)-N-[3-[[4-(trifluoromethyl)-1-piperidinyl]methyl]-5-isothiazolyl]imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C20H22ClF3N8S
 1
1 IC50 <= 13 nM
CP0712128
2-Methyl-2-[[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-isothiazolyl]methyl](2,2,2-trifluoroethyl)amino]-1-propanol Hydrochloride
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C20H24ClF3N8OS
 1
1 IC50 <= 13 nM
CP0751381
N-[3-[(3-Fluoro-1-azetidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Trifluoroacetate
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C19H18F4N8O2S
 1
1 IC50 <= 13 nM
CP0784483
N-[3-[(3-Fluoro-1-piperidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H22ClFN8S
 1
1 IC50 <= 13 nM
CP0790429
N-[3-[(3,3-Difluoro-1-piperidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H21ClF2N8S
 1
1 IC50 <= 13 nM
CP0802122
N-[3-[(3,3-Difluoro-1-azetidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Trifluoroacetate
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C19H17F5N8O2S
 1
1 IC50 <= 13 nM
CP0814301
N-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)-3-(pyrrolidin-1-ylmethyl)isothiazol-5-amine Hydrochloride
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C18H21ClN8S
 1
1 IC50 <= 13 nM
CP0817001
N-[3-[(3(S)-Fluoro-1-pyrrolidinyl)methyl]-5-isothiazolyl]-6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C18H20ClFN8S
 1
1 IC50 <= 13 nM
CP0105279
6-Methyl-N-[3-(1-piperidinylmethyl)-5-isothiazolyl]-3-(1Hpyrazol-4-yl)imidazo[1,2-a]pyrazin-8-amine Hydrochloride
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C19H22N8S
 2
1 IC50 < 13 nM
2 IC50 <= 13 nM
CP0105267
N-(2,3-difluorophenyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H27F2N9OS
 1
1 IC50 <= 13 nM
CP0105278
N-[(4-fluorophenyl)methyl]-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C28H30FN9OS
 1
1 IC50 <= 13 nM
CP0125882
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-pyridin-4-ylacetamide
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C27H30N10OS
 1
1 IC50 <= 13 nM
CP0146469
N-[6-methyl-3-[1-[(3-phenyl-1,2,4-oxadiazol-5-yl)methyl]pyrazol-4-yl]imidazo[1,2-a]pyrazin-8-yl]-3-(piperidin-1-ylmethyl)-1,2-thiazol-5-amine
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C28H28N10OS
 1
1 IC50 <= 13 nM
CP0146474
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-(thiophen-2-ylmethyl)acetamide
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C27H31N9OS2
 1
1 IC50 <= 13 nM
CP0181883
N-[(2-fluorophenyl)methyl]-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C28H30FN9OS
 1
1 IC50 <= 13 nM
CP0248286
N-(3-fluoropyridin-4-yl)-2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H29FN10OS
 1
1 IC50 <= 13 nM
CP0248287
N-[(3-fluorophenyl)methyl]-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C28H30FN9OS
 1
1 IC50 <= 13 nM
CP0248288
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-(1,3-thiazol-2-yl)acetamide
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C25H28N10OS2
 1
1 IC50 <= 13 nM
CP0248304
N-[3-[1-(1H-benzimidazol-2-ylmethyl)pyrazol-4-yl]-6-methylimidazo[1,2-a]pyrazin-8-yl]-3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-amine
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C28H30N10S
 1
1 IC50 <= 13 nM
CP0333218
N-(3-fluorophenyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H28FN9OS
 1
1 IC50 <= 13 nM
CP0333907
N-benzyl-2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C29H33N9OS
 1
1 IC50 <= 13 nM
CP0338008
N-[(2,3-difluorophenyl)methyl]-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C28H29F2N9OS
 1
1 IC50 <= 13 nM
CP0340347
N-[(3,5-difluorophenyl)methyl]-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C28H29F2N9OS
 1
1 IC50 <= 13 nM
CP0517504
N-[6-methyl-3-[1-[(5-phenyl-1,2,4-oxadiazol-3-yl)methyl]pyrazol-4-yl]imidazo[1,2-a]pyrazin-8-yl]-3-(piperidin-1-ylmethyl)-1,2-thiazol-5-amine
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C28H28N10OS
 1
1 IC50 <= 13 nM
CP0068126
2-[ethyl-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]amino]ethanol
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C18H22N8OS
 1
1 IC50 < 13 nM
CP0080498
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyrimidin-2-ylmethyl)-1,2-thiazol-5-amine
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C18H15N9S
 1
1 IC50 < 13 nM
CP0080506
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[(3-methylpyridin-2-yl)methyl]-1,2-thiazol-5-amine
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C20H18N8S
 1
1 IC50 < 13 nM
CP0101516
3-[(6-methoxypyridin-2-yl)methyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C20H18N8OS
 1
1 IC50 < 13 nM
CP0101517
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[(5-methylpyridin-2-yl)methyl]-1,2-thiazol-5-amine
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C20H18N8S
 1
1 IC50 < 13 nM
CP0101571
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[pyridin-2-yl(pyrrolidin-1-yl)methyl]-1,2-thiazol-5-amine
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C23H23N9S
 1
1 IC50 < 13 nM
CP0101572
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[(4-methylpyridin-2-yl)methyl]-1,2-thiazol-5-amine
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C20H18N8S
 1
1 IC50 < 13 nM
CP0102956
[6-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]pyridin-2-yl]-piperidin-1-ylmethanone
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C25H25N9OS
 1
1 IC50 < 13 nM
CP0102957
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyridin-2-ylmethyl)-1,2-thiazol-5-amine
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C19H16N8S
 2
1 IC50 < 13 nM
2 Kd = 0.1 nM
CP0225496
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyridin-4-ylmethyl)-1,2-thiazol-5-amine
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C19H16N8S
 1
1 IC50 < 13 nM
CP0225497
3-(imidazol-1-ylmethyl)-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C17H15N9S
 1
1 IC50 < 13 nM
CP0225498
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(1,3-thiazol-2-ylmethyl)-1,2-thiazol-5-amine
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C17H14N8S2
 1
1 IC50 < 13 nM
CP0225500
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[piperidin-1-yl(pyridin-2-yl)methyl]-1,2-thiazol-5-amine
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C24H25N9S
 1
1 IC50 < 13 nM
CP0311219
3-[(4-fluoropiperidin-1-yl)-pyridin-2-ylmethyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C24H24FN9S
 1
1 IC50 < 13 nM
CP0323338
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[[6-(piperidin-1-ylmethyl)pyridin-2-yl]methyl]-1,2-thiazol-5-amine
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C25H27N9S
 1
1 IC50 < 13 nM
CP0329737
3-methyl-1-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]pyridin-2-one
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C20H18N8OS
 1
1 IC50 < 13 nM
CP0329738
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyrazol-1-ylmethyl)-1,2-thiazol-5-amine
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C17H15N9S
 1
1 IC50 < 13 nM
CP0329739
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-[(6-methylpyridin-2-yl)methyl]-1,2-thiazol-5-amine
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C20H18N8S
 1
1 IC50 < 13 nM
CP0340785
3-[(3-fluoropyridin-2-yl)methyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C19H15FN8S
 1
1 IC50 < 13 nM
CP0364547
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyrazin-2-ylmethyl)-1,2-thiazol-5-amine
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C18H15N9S
 1
1 IC50 < 13 nM
CP0364548
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyrrol-1-ylmethyl)-1,2-thiazol-5-amine
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C18H16N8S
 1
1 IC50 < 13 nM
CP0364549
[6-[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-1,2-thiazol-3-yl]methyl]pyridin-2-yl]methanol
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C20H18N8OS
 1
1 IC50 < 13 nM
CP0364550
3-[(5-fluoropyridin-2-yl)methyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C19H15FN8S
 1
1 IC50 < 13 nM
CP0404218
N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-3-(pyridin-3-ylmethyl)-1,2-thiazol-5-amine
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C19H16N8S
 1
1 IC50 < 13 nM
CP0469385
3-[(cyclopentylamino)-pyridin-2-ylmethyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C24H25N9S
 1
1 IC50 < 13 nM
CP0564662
3-[(6-fluoropyridin-2-yl)methyl]-N-[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine
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C19H15FN8S
 1
1 IC50 < 13 nM
CP0018039
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C23H28N8OS
 14
1 IC50 = 14.7 nM
2 IC50 = 15.7 nM
3 IC50 = 17 nM
4 IC50 = 18 nM
5 IC50 = 18.6 nM
6 IC50 = 30 nM
7 IC50 = 40 nM
8 IC50 = 43 nM
9 IC50 = 68 nM
10 Kd = 7 nM
11 Kd = 7.4 nM
12 Ki = 1.8 nM
13 Ki = 3.36 nM
14 Ki = 18 nM
CP0025073
4-(4-Fluorophenyl)-N-(4-(3-(2-(methylamino)pyrimidin-4-yl)-pyridin-2-yloxy)phenyl)phthalazin-1-amine
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C30H22FN7O
 1
1 IC50 = 15 nM
CP0026408
2-anilino-N-[3-methyl-4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]benzamide
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C30H26N6O2
 1
1 IC50 = 17 nM
CP0110915
N-[6-methyl-3-[1-[(5-phenyl-1H-imidazol-2-yl)methyl]pyrazol-4-yl]imidazo[1,2-a]pyrazin-8-yl]-3-(piperidin-1-ylmethyl)-1,2-thiazol-5-amine
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C29H30N10S
 1
1 IC50 = 21 nM
CP0015614
N-[4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]-4-phenylphthalazin-1-amine
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C30H23N7O
 1
1 IC50 = 22 nM
CP0238983
Bisanilinopyrimidine, 9j
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C20H19ClFN5O
 1
1 IC50 = 25.6 nM
CP0061157
N-[4-(1,3-benzothiazol-2-yl)-3-fluorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 27 nM
CP0151244
N-[4-(1,3-benzothiazol-2-yl)-2-fluorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 28 nM
CP0146467
2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C21H25N9OS
 1
1 IC50 = 28 nM
CP0333908
N-(6-fluoropyridin-2-yl)-2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H29FN10OS
 1
1 IC50 = 28 nM
CP0125881
N-(4-fluorophenyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H28FN9OS
 1
1 IC50 = 30 nM
CP0318290
Bisanilinopyrimidine, 9k
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C21H21ClFN5O
 1
1 IC50 = 30 nM
CP0338488
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-pyridin-2-ylacetamide
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C27H30N10OS
 1
1 IC50 = 32 nM
CP0110916
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-[[3-(trifluoromethyl)phenyl]methyl]acetamide
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C30H32F3N9OS
 1
1 IC50 = 35 nM
CP0176075
N-(2-fluorophenyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H28FN9OS
 1
1 IC50 = 35 nM
CP0267380
Bisanilinopyrimidine, 9l
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C19H18ClN5O2
 1
1 IC50 = 40.4 nM
CP0069712
N-[4-(6-fluoro-1,3-benzothiazol-2-yl)phenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 41 nM
CP0176074
N-[(3-methoxyphenyl)methyl]-2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C30H35N9O2S
 1
1 IC50 = 41 nM
CP0168034
4-[(7-hydroxy-6-methoxyquinazolin-4-yl)amino]-N-phenylbenzamide
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C22H18N4O3
 1
1 IC50 = 41 nM
CP0314266
Bisanilinopyrimidine, 9i
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C16H14ClN5O2S
 1
1 IC50 = 43.3 nM
CP0333195
N-(3-methylbutyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C26H35N9OS
 1
1 IC50 = 44 nM
CP0181888
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-(3H-pyridazin-2-yl)acetamide
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C26H31N11OS
 1
1 IC50 = 45 nM
CP0284644
Bisanilinopyrimidine, 6p
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C17H14ClN5O
 1
1 IC50 = 50.2 nM
CP0181858
2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]-N-phenylacetamide
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C28H31N9OS
 1
1 IC50 = 51 nM
CP0016235
N-[3-methyl-4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]-2-phenoxybenzamide
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C30H25N5O3
 1
1 IC50 = 56 nM
CP0103207
Bisanilinopyrimidine, 9n
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C16H13ClFN5O2S
 1
1 IC50 = 56.6 nM
CP0151301
2-(1,3-benzothiazol-2-yl)-5-[[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]amino]phenol
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C30H32N6O3S
 1
1 IC50 = 59 nM
CP0091117
N-[4-(5-chloro-1,3-benzothiazol-2-yl)phenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31ClN6O2S
 1
1 IC50 = 62 nM
CP0015507
2-(4-(6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
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C30H31N5O3S
 1
1 IC50 = 63 nM
CP0023880
N-[3-methyl-4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]-3-(trifluoromethyl)benzamide
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C25H20F3N5O2
 1
1 IC50 = 66 nM
CP0166275
N-[4-(1,3-benzothiazol-2-yl)-3-chlorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31ClN6O2S
 1
1 IC50 = 78 nM
CP0327179
N-(2-fluoropyridin-3-yl)-2-[4-[6-methyl-8-[[3-[(3-methylpiperidin-1-yl)methyl]-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H29FN10OS
 1
1 IC50 = 81 nM
CP0274623
Bisanilinopyrimidine, 12b
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C17H12ClFN8
 1
1 IC50 = 83.7 nM
CP0151259
N-[4-(1,3-benzothiazol-2-yl)-2-methoxyphenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C31H34N6O3S
 1
1 IC50 = 90 nM
CP0032546
4-(9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-ylamino)-2-methoxybenzoic acid
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C27H20ClFN4O4
 5
1 IC50 = 90 nM
2 IC50 = 396 nM
3 IC50 = 396.5 nM
4 IC50 = 1100 nM
5 IC50 > 200 nM
CP0675722
4-(2-(4-(6-methyl-8-(3-((3-methylpiperidin-1-yl)methyl)isothiazol-5-ylamino)imidazo[1,2-a]pyrazin-3-yl)-1H-pyrazol-1-yl)acetamido)pyridine 1-oxide
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C27H30N10O2S
 1
1 IC50 = 91 nM
CP0193836
Bisanilinopyrimidine, 9b
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C21H23ClN6O
 1
1 IC50 = 93.9 nM
CP0248307
N-(3,5-difluorophenyl)-2-[4-[6-methyl-8-[[3-(piperidin-1-ylmethyl)-1,2-thiazol-5-yl]amino]imidazo[1,2-a]pyrazin-3-yl]pyrazol-1-yl]acetamide
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C27H27F2N9OS
 1
1 IC50 = 94 nM
CP0356087
Bisanilinopyrimidine, 12d
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C17H12Cl2N8
 1
1 IC50 = 106 nM
CP0020460
2-anilino-N-[2-methyl-4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]benzamide
   Show/Hide
C30H26N6O2
 1
1 IC50 = 110 nM
CP0128578
6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]-N-[4-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]phenyl]quinazolin-4-amine
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C31H31F3N6O2S
 1
1 IC50 = 120 nM
CP0147199
Bisanilinopyrimidine, 9c
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C20H20ClN5O2
 1
1 IC50 = 123 nM
CP0015511
2-[3-fluoro-4-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]oxyphenyl]-1,3-benzothiazole
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C30H30FN5O3S
 1
1 IC50 = 130 nM
CP0051782
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazole 18
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C28H35N7O2
 1
1 IC50 = 135 nM
CP0016366
2-(4-(6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
   Show/Hide
C29H28N4O3S
 1
1 IC50 = 162 nM
CP0017774
4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid
   Show/Hide
C25H15ClF2N4O2
 2
1 IC50 = 172 nM
2 Kd = 43 nM
CP0247099
Bisanilinopyrimidine, 9e
   Show/Hide
C18H16ClN5O
 1
1 IC50 = 174 nM
CP0170069
Bisanilinopyrimidine, 9d
   Show/Hide
C17H15ClN4O2S
 1
1 IC50 = 180 nM
CP0267383
Bisanilinopyrimidine, 9h
   Show/Hide
C20H20ClN5O
 1
1 IC50 = 194 nM
CP0117152
Bisanilinopyrimidine, 12a
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C17H13ClN8
 1
1 IC50 = 226 nM
CP0301029
Bisanilinopyrimidine, 9a
   Show/Hide
C23H25ClN6O2
 1
1 IC50 = 232 nM
CP0020487
N-[3-methyl-4-[3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl]oxyphenyl]-3-phenoxybenzamide
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C30H25N5O3
 1
1 IC50 = 251 nM
CP0135618
N-[4-(1,3-benzothiazol-2-yl)-3-methoxyphenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C31H34N6O3S
 1
1 IC50 = 300 nM
CP0026752
4-Chloro-N-(3-methyl-4-(3-(2-(methylamino)pyrimidin-4-yl)-pyridin-2-yloxy)phenyl)benzamide
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C24H20ClN5O2
 1
1 IC50 = 335 nM
CP0704813
N4-(2-Chlorophenyl)-N2-[6-(1H-benzo[d]imidazol-2(3H)-one)]pyrimidine-2,4-diamine
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C17H13ClN6O
 1
1 IC50 = 361 nM
CP0019760
3-Chloro-N-(3-methyl-4-(3-(2-(methylamino)pyrimidin-4-yl)-pyridin-2-yloxy)phenyl)benzamide
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C24H20ClN5O2
 1
1 IC50 = 430 nM
CP0296124
4-[[6-chloro-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]oxy]-N-(3-methyl-1,2-oxazol-5-yl)benzamide
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C22H18ClN7O3
 1
1 IC50 = 693 nM
CP0157791
Bisanilinopyrimidine, 9g
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C18H15ClN4O3
 1
1 IC50 = 1510 nM
CP0026997
Alternariol
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C14H10O5
 1
1 IC50 = 1626.457034 nM
CP0204584
4-[[6-chloro-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]oxy]-N-pyridin-3-ylbenzamide
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C23H18ClN7O2
 1
1 IC50 = 1676 nM
CP0075920
4-[[6-chloro-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]oxy]-N-cyclobutylbenzamide
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C22H21ClN6O2
 1
1 IC50 = 3045 nM
CP0296123
4-[[6-chloro-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]oxy]-N-pyridin-4-ylbenzamide
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C23H18ClN7O2
 1
1 IC50 = 3447 nM
CP0270630
4-[[6-chloro-2-(1,3-dimethylpyrazol-4-yl)-1H-imidazo[4,5-b]pyridin-7-yl]oxy]-N-phenylbenzamide
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C24H19ClN6O2
 1
1 IC50 = 12710 nM
CP0203400
2-[(3S,4S)-3-fluoro-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C22H23FN8O2S
 1
1 Kd = 1 nM
CP0120735
2-[(3R)-3-(2-hydroxyethoxy)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C24H28N8O3S
 1
1 Kd = 1.7 nM
CP0178025
2-[(3R)-3-(3,3-difluoropyrrolidine-1-carbonyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H29F2N9O2S
 1
1 Kd = 1.7 nM
CP0178029
(3R)-N-cyclopentyl-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]pyrrolidine-3-carboxamide
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C28H33N9O2S
 1
1 Kd = 1.9 nM
CP0178032
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3S)-3-(pyrrolidine-1-carbonyl)pyrrolidin-1-yl]acetamide
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C27H31N9O2S
 1
1 Kd = 1.9 nM
CP0203396
2-[(3S,4S)-3-(cyclopropylmethoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H30N8O3S
 1
1 Kd = 2 nM
CP0203398
2-[(3S,4S)-3-hydroxy-4-(2-methoxyethoxy)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C25H30N8O4S
 1
1 Kd = 2 nM
CP0256641
(3R)-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]-N-(2,2,2-trifluoroethyl)pyrrolidine-3-carboxamide
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C25H26F3N9O2S
 1
1 Kd = 2.2 nM
CP0767144
rac-N-(4-((4-((5-Methyl-1H-pyrazol-3-yl)amino)pyrrolo[2,1-f][1,2,4]triazin-2-yl)thio)phenyl)-2-(3-(pyrrolidine-1-carbonyl)pyrrolidin-1-yl)acetamide
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C27H31N9O2S
 1
1 Kd = 2.4 nM
CP0178031
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3R)-3-(pyrrolidine-1-carbonyl)pyrrolidin-1-yl]acetamide
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C27H31N9O2S
 1
1 Kd = 2.5 nM
CP0153379
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3R)-3-(morpholine-4-carbonyl)pyrrolidin-1-yl]acetamide
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C27H31N9O3S
 1
1 Kd = 2.6 nM
CP0087504
(3R)-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]-N-(2-morpholin-4-ylethyl)pyrrolidine-3-carboxamide
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C29H36N10O3S
 1
1 Kd = 2.9 nM
CP0160241
2-[(3R)-3-[2-(4-methylpiperazin-1-yl)ethoxy]pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C29H38N10O2S
 1
1 Kd = 2.9 nM
CP0199882
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3R)-3-(piperidine-1-carbonyl)pyrrolidin-1-yl]acetamide
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C28H33N9O2S
 1
1 Kd = 2.9 nM
CP0120734
2-[(3R)-3-(2-methoxyethoxy)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C25H30N8O3S
 1
1 Kd = 3.1 nM
CP0160243
(3R)-N-tert-butyl-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]pyrrolidine-3-carboxamide
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C27H33N9O2S
 1
1 Kd = 3.1 nM
CP0256639
2-[(3R)-3-tert-butylsulfinylpyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H32N8O2S2
 1
1 Kd = 3.1 nM
CP0208183
2-[(3R)-3-(methanesulfonamido)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H27N9O3S2
 1
1 Kd = 3.2 nM
CP0084970
(3R)-N-cyclobutyl-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]pyrrolidine-3-carboxamide
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C27H31N9O2S
 1
1 Kd = 3.3 nM
CP0208185
2-[(3R)-3-[(2-methylpropan-2-yl)oxy]pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H32N8O2S
 1
1 Kd = 3.6 nM
CP0178030
2-[(3R)-3-(4-hydroxypiperidine-1-carbonyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H33N9O3S
 1
1 Kd = 3.7 nM
CP0256640
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3R)-3-(3-morpholin-4-ylpropoxy)pyrrolidin-1-yl]acetamide
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C29H37N9O3S
 1
1 Kd = 3.7 nM
CP0203395
2-[(3S,4S)-3-cyclopentyloxy-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H32N8O3S
 1
1 Kd = 4 nM
CP0203397
2-[(3S,4S)-3-hydroxy-4-propan-2-yloxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C25H30N8O3S
 1
1 Kd = 4 nM
CP0203408
2-[(2S,4S)-4-fluoro-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H25FN8O2S
 1
1 Kd = 4 nM
CP0232139
N-[4-[6-[[2-(4-methylpiperazin-1-yl)-2-oxoacetyl]amino]-4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C27H30N10O3S
 1
1 Kd = 4 nM
CP0255607
2-[(3S,4S)-3-hydroxy-4-(2-methylbutan-2-yloxy)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H34N8O3S
 1
1 Kd = 4 nM
CP0299339
2-[(3S,4S)-3-hydroxy-4-(1,1,1-trifluoro-2-methylpropan-2-yl)oxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H29F3N8O3S
 1
1 Kd = 4 nM
CP0299340
2-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H26N8O2S
 1
1 Kd = 4 nM
CP0078576
2-[(3R)-3-tert-butylsulfonylpyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H32N8O3S2
 1
1 Kd = 4.3 nM
CP0297797
2-[(2S)-4,4-difluoro-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H24F2N8O2S
 1
1 Kd = 5 nM
CP0314104
2-[(3S,4S)-3-hydroxy-4-[(2-methylpropan-2-yl)oxy]pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H32N8O3S
 1
1 Kd = 5 nM
CP0713838
E/Z-(S,E)-2-(3-tert-butoxy-4-(hydroxyimino)pyrrolidin-1-yl)-N-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-ylthio)phenyl)acetamide
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C26H31N9O3S
 1
1 Kd = 5 nM
CP0315665
2-methyl-N-[(3R)-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]pyrrolidin-3-yl]propanamide
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C26H31N9O2S
 1
1 Kd = 5.7 nM
CP0120732
2-[3-(2,2-dimethylpropanoyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H32N8O2S
 1
1 Kd = 6.1 nM
CP0120733
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-[(3R)-3-(2-morpholin-4-ylethoxy)pyrrolidin-1-yl]acetamide
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C28H35N9O3S
 1
1 Kd = 6.6 nM
CP0178027
2-[(3R)-3-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C22H24N8O2S
 1
1 Kd = 6.6 nM
CP0084971
(3R)-N-(4-fluorophenyl)-1-[2-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylanilino]-2-oxoethyl]pyrrolidine-3-carboxamide
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C29H28FN9O2S
 1
1 Kd = 6.9 nM
CP0180529
2-[(3S,4S)-3-(4-fluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H27FN8O3S
 1
1 Kd = 8 nM
CP0255608
2-(dimethylamino)-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C20H22N8OS
 1
1 Kd = 8 nM
CP0271602
2-[(3S,4R)-3-(4-fluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H27FN8O3S
 1
1 Kd = 8 nM
CP0297798
2-[(2S,4R)-2-(hydroxymethyl)-4-[(2-methylpropan-2-yl)oxy]pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H34N8O3S
 1
1 Kd = 8 nM
CP0203409
2-[(2S,4R)-4-fluoro-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H25FN8O2S
 1
1 Kd = 9 nM
CP0232138
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]-6-[(2-morpholin-4-ylacetyl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C26H29N9O3S
 1
1 Kd = 9 nM
CP0305823
2-[(3S,4S)-3-(2-fluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H27FN8O3S
 1
1 Kd = 9 nM
CP0203394
2-[(3S,4S)-3-(3-fluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H27FN8O3S
 1
1 Kd = 10 nM
CP0334840
2-[(3R)-3-tert-butylsulfanylpyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C26H32N8OS2
 1
1 Kd = 14.2 nM
CP0314405
2-[(3S)-3-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C22H24N8O2S
 1
1 Kd = 14.8 nM
CP0203402
2-[(2S,4R)-4-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H26N8O3S
 1
1 Kd = 15 nM
CP0203406
2-[(1R,2S,5S)-2-(hydroxymethyl)-3-azabicyclo[3.1.0]hexan-3-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C24H26N8O2S
 1
1 Kd = 15 nM
CP0271591
N-[4-[6-[[2-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]acetyl]amino]-4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C27H31N9O3S
 1
1 Kd = 16 nM
CP0299338
2-[(3S,4S)-3-(2,4-difluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H26F2N8O3S
 1
1 Kd = 17 nM
CP0235845
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C20H19N7OS
 1
1 Kd = 20 nM
CP0203404
2-[(2S,4R)-4-(4-fluorophenoxy)-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C29H29FN8O3S
 1
1 Kd = 21 nM
CP0305822
2-[(3S,4S)-3-(3,5-difluorophenoxy)-4-hydroxypyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C28H26F2N8O3S
 1
1 Kd = 21 nM
CP0235846
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]-6-(3-piperidin-1-ylpropanoylamino)pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C28H33N9O2S
 1
1 Kd = 37 nM
CP0252947
2-[(2S,4R)-4-tert-butylsulfanyl-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H34N8O2S2
 1
1 Kd = 39 nM
CP0203410
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]-2-morpholin-4-ylacetamide
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C22H24N8O2S
 1
1 Kd = 41 nM
CP0252950
2-(cyclopropylamino)-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C21H22N8OS
 1
1 Kd = 41 nM
CP0164886
2-(cyclopentylamino)-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H26N8OS
 1
1 Kd = 42 nM
CP0088050
US9447092, 1
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C22H23Cl2N7
 1
1 Kd = 48 nM
CP0235848
N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]-6-[(2-pyrrolidin-1-ylacetyl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
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C26H29N9O2S
 1
1 Kd = 49 nM
CP0248466
2-[(2R,4R)-2-(hydroxymethyl)-4-[(2-methylpropan-2-yl)oxy]pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C27H34N8O3S
 1
1 Kd = 69 nM
CP0248465
2-[(2S,4R)-4-amino-2-(hydroxymethyl)pyrrolidin-1-yl]-N-[4-[4-[(5-methyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]sulfanylphenyl]acetamide
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C23H27N9O2S
 1
1 Kd = 144 nM
Clinical Information about the Protein
Target 1 ( Aurora kinase B (AURKB) )
Target Type Clinical trial Target
Disease 6 Target-related Diseases  6
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Haematological malignancy [ICD-11: 2B33.Y]
3 Prostate cancer [ICD-11: 2C82.0]
4 Advanced solid tumour [ICD-11: 2A00-2F9Z]
5 Diabetic complication [ICD-11: 5A2Y]
6 Esophageal squamous cell carcinoma [ICD-11: 2E60.1]
Clinical Trial Drug(s) 13 Clinical Trial Drugs  13
1 AT9283 Phase 3
Solid tumour/cancer
2 ABT-348 Phase 2
Haematological malignancy
3 PHA-739358 Phase 2
Prostate cancer
4 VX-680 Phase 2
Solid tumour/cancer
5 AMG 900 Phase 1
Solid tumour/cancer
6 AZD-1152-HQPA Phase 1
Solid tumour/cancer
7 CYC116 Phase 1
Solid tumour/cancer
8 GSK1070916 Phase 1
Advanced solid tumour
9 MK-5108 Phase 1
Solid tumour/cancer
10 R763 Phase 1
Haematological malignancy
11 Rosiglitazone + metformin Phase 3
Diabetic complication
12 SNS-314 Phase 1
Solid tumour/cancer
13 TAK-901 Phase 1
Haematological malignancy
Discontinued Drug(s) 1 Discontinued Drug  1
1 PF-03814735 Discontinued in Phase 1
Advanced solid tumour
Investigative Drug(s) 1 Investigative Drug  1
1 Deguelin Investigative
Esophageal squamous cell carcinoma
Target 2 ( Aurora B messenger RNA (AURKB mRNA) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Prostate cancer [ICD-11: 2C82.0]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PHA-739358 Phase 2
Prostate cancer