General Information of the Protein
Protein ID
PT00980
Protein Name
Aurora kinase A
Secondarily
Protein Name
Aurora 2
Aurora/IPL1-related kinase 1
Breast tumor-amplified kinase
Ipl1- and aurora-related kinase 1
Serine/threonine-protein kinase 15
Serine/threonine-protein kinase 6
Serine/threonine-protein kinase Ayk1
Serine/threonine-protein kinase aurora-A
Gene Name
AURKA
Secondarily
Gene Name
AIK
AIRK1
ARK1
AURA
AYK1
BTAK
IAK1
STK15
STK6
Sequence
MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRIPLQAQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKNEESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRREVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITELANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEMIEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLISRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Other protein kinase group
>
Other protein kinase AUR family
Function
Mitotic serine/threonine kinase that contributes to the regulation of cell cycle progression (PubMed:26246606, PubMed:12390251, PubMed:18615013, PubMed:11039908, PubMed:17125279, PubMed:17360485). Associates with the centrosome and the spindle microtubules during mitosis and plays a critical role in various mitotic events including the establishment of mitotic spindle, centrosome duplication, centrosome separation as well as maturation, chromosomal alignment, spindle assembly checkpoint, and cytokinesis (PubMed:26246606, PubMed:14523000). Required for normal spindle positioning during mitosis and for the localization of NUMA1 and DCTN1 to the cell cortex during metaphase (PubMed:27335426). Required for initial activation of CDK1 at centrosomes (PubMed:13678582, PubMed:15128871). Phosphorylates numerous target proteins, including ARHGEF2, BORA, BRCA1, CDC25B, DLGP5, HDAC6, KIF2A, LATS2, NDEL1, PARD3, PPP1R2, PLK1, RASSF1, TACC3, p53/TP53 and TPX2 (PubMed:18056443, PubMed:15128871, PubMed:14702041, PubMed:11551964, PubMed:15147269, PubMed:15987997, PubMed:17604723, PubMed:18615013). Regulates KIF2A tubulin depolymerase activity (PubMed:19351716). Important for microtubule formation and/or stabilization (PubMed:18056443). Required for normal axon formation (PubMed:19812038). Plays a role in microtubule remodeling during neurite extension (PubMed:19668197). Also acts as a key regulatory component of the p53/TP53 pathway, and particularly the checkpoint-response pathways critical for oncogenic transformation of cells, by phosphorylating and destabilizing p53/TP53 (PubMed:14702041). Phosphorylates its own inhibitors, the protein phosphatase type 1 (PP1) isoforms, to inhibit their activity (PubMed:11551964). Inhibits cilia outgrowth (By similarity). Required for cilia disassembly via phosphorylation of HDAC6 and subsequent deacetylation of alpha-tubulin (PubMed:17604723, PubMed:20643351). Regulates protein levels of the anti-apoptosis protein BIRC5 by suppressing the expression of the SCF(FBXL7) E3 ubiquitin-protein ligase substrate adapter FBXL7 through the phosphorylation of the transcription factor FOXP1 (PubMed:28218735).
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Uniprot ID
Primary ID:
O14965

Secondarily ID:
E1P5F9
O60445
O75873
Q9BQD6
Q9UPG5
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Ensembl ID
ENSG00000087586
HGNC ID
HGNC:11393
Subcellular Location
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Cytoplasm
Cytoskeleton
Spindle pole
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Centriole
Cell projection
Neuron projection
Cell projection
Cilium
Cytoplasm
Cytoskeleton
Cilium basal body
Basolateral cell membrane
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
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 = 13 nM
   TI
   LI
   LO
   TS
CP0470449
N-[6-methyl-3-[(E)-2-phenylethenyl]-1H-indazol-5-yl]-2-thiophen-2-ylacetamide
   Show/Hide
C22H19N3OS
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0490727
N-[6-methyl-3-[(E)-2-phenylethenyl]-1H-indazol-5-yl]-2-phenylacetamide
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C24H21N3O
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0486037
2-phenyl-N-(3-styryl-1H-indazol-5-yl)acetamide
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C23H19N3O
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0376394
1-phenyl-N-(3-styryl-1H-indazol-5-yl)methanesulfonamide
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C22H19N3O2S
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
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 = 35 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 = 42 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 = 79 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 = 91 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 = 140 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 = 160 nM
   TI
   LI
   LO
   TS
CP0477501
6-(pyrrolidin-1-yl)-3-styryl-1H-indazol-5-amine
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C19H20N4
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0376393
5-nitro-6-(pyrrolidin-1-yl)-3-styryl-1H-indazole
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C19H18N4O2
 1
1
IC50 = 240 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 = 240 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 = 280 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 = 350 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 = 620 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 = 640 nM
   TI
   LI
   LO
   TS
CP0417626
2-phenyl-N-[3-(2-phenylethyl)-2H-indazol-5-yl]acetamide
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C23H21N3O
 1
1
IC50 = 1700 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 = 1900 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 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0361417
CHEMBL4563026
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C33H34ClFN7O3
 1
1 IC50 = 0.06 nM
CP0016524
CHEMBL3600873
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C22H21ClFN3O3S
 1
1 IC50 = 0.064 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
 25
1 IC50 = 0.24 nM
2 IC50 = 0.6 nM
3 IC50 = 0.7 nM
4 IC50 = 0.95 nM
5 IC50 = 1.05 nM
6 IC50 = 1.4 nM
7 IC50 = 1.9 nM
8 IC50 = 2.8 nM
9 IC50 = 6 nM
10 IC50 = 15 nM
11 IC50 = 20 nM
12 IC50 = 30 nM
13 IC50 = 31.62 nM
14 IC50 = 127 nM
15 IC50 = 130 nM
16 Kd = 0.3333 nM
17 Kd = 0.645 nM
18 Kd = 3.9 nM
19 Kd = 4 nM
20 Kd = 4.1 nM
21 Kd = 17 nM
22 Ki = 0.37 nM
23 Ki = 0.6 nM
24 Ki = 0.65 nM
25 Ki = 1 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 21
1 IC50 = 0.46 nM
2 IC50 = 0.6 nM
3 IC50 = 0.86 nM
4 IC50 = 0.936 nM
5 IC50 <= 1 nM
6 IC50 < 1 nM
7 IC50 = 1.38 nM
8 IC50 = 2 nM
9 IC50 = 2.28 nM
10 IC50 = 2.4 nM
11 IC50 = 3 nM
12 IC50 = 3.67 nM
13 IC50 = 7.63 nM
14 IC50 = 11 nM
15 IC50 = 15 nM
16 IC50 = 18.09 nM
17 IC50 = 22 nM
18 IC50 = 23 nM
19 Kd = 16 nM
20 Kd = 17 nM
21 Kd = 110 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 = 0.6 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
 3
1 IC50 = 1 nM
2 IC50 = 1.2 nM
3 IC50 = 100 nM
CP0017774
4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid
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C25H15ClF2N4O2
 5
1 IC50 = 1.5 nM
2 IC50 = 4 nM
3 Kd = 0.3467 nM
4 Kd = 0.9133 nM
5 Kd = 6.5 nM
CP0274623
Bisanilinopyrimidine, 12b
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C17H12ClFN8
 1
1 IC50 = 2.9 nM
CP0356087
Bisanilinopyrimidine, 12d
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C17H12Cl2N8
 1
1 IC50 = 3 nM
CP0117152
Bisanilinopyrimidine, 12a
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C17H13ClN8
 2
1 IC50 = 3.1 nM
2 Kd = 18 nM
CP0037005
2,4-Bisanilinopyrimidine, 10
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C31H31ClFN7O2
 1
1 IC50 = 3.4 nM
CP0182104
Bisanilinopyrimidine inhibitor, 2
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C18H14N4O4
 4
1 IC50 = 5.1 nM
2 IC50 = 6.1 nM
3 IC50 = 75 nM
4 Kd = 34 nM
CP0267380
Bisanilinopyrimidine, 9l
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C19H18ClN5O2
 1
1 IC50 = 12.3 nM
CP0025009
Bisanilinopyrimidine, 9m
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C17H13ClFN5O
 1
1 IC50 = 14.4 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 = 15 nM
CP0365386
Bisanilinopyrimidine, 12c
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C17H12ClFN8O
 1
1 IC50 = 17.3 nM
CP0147199
Bisanilinopyrimidine, 9c
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C20H20ClN5O2
 1
1 IC50 = 18 nM
CP0103207
Bisanilinopyrimidine, 9n
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C16H13ClFN5O2S
 1
1 IC50 = 21.2 nM
CP0238983
Bisanilinopyrimidine, 9j
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C20H19ClFN5O
 1
1 IC50 = 21.4 nM
CP0318290
Bisanilinopyrimidine, 9k
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C21H21ClFN5O
 1
1 IC50 = 23.2 nM
CP0051782
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazole 18
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C28H35N7O2
 3
1 IC50 = 27 nM
2 Kd = 1.84 nM
3 Kd = 2.613 nM
CP0267383
Bisanilinopyrimidine, 9h
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C20H20ClN5O
 1
1 IC50 = 27 nM
CP0301029
Bisanilinopyrimidine, 9a
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C23H25ClN6O2
 1
1 IC50 = 28.1 nM
CP0284644
Bisanilinopyrimidine, 6p
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C17H14ClN5O
 1
1 IC50 = 30.2 nM
CP0170069
Bisanilinopyrimidine, 9d
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C17H15ClN4O2S
 1
1 IC50 = 44.9 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 = 58 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 = 67 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 = 71 nM
CP0173802
4-(6,7-Dimethoxy-9H-pyrimido[4,5-b]indol-4-yl)-piperazine-1-carbothioic acid [4-(pyrimidin-2-ylsulfamoyl)-phenyl]-amide
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C27H27N9O4S2
 2
1 IC50 = 94 nM
2 IC50 = 900 nM
CP0157791
Bisanilinopyrimidine, 9g
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C18H15ClN4O3
 1
1 IC50 = 116.5 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 = 190 nM
CP0193836
Bisanilinopyrimidine, 9b
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C21H23ClN6O
 1
1 IC50 = 216 nM
CP0230489
CHEMBL4763626
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C18H16ClN5O5
 1
1 IC50 = 222 nM
CP0314266
Bisanilinopyrimidine, 9i
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C16H14ClN5O2S
 1
1 IC50 = 253 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 = 316 nM
CP0036099
1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea
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C21H18FN5O
 2
1 IC50 = 760 nM
2 Kd = 1600 nM
CP0634648
N-((R)-Cyclopropyl(pyridin-2-yl)methyl)-3-(4-((endo)-3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl)phenyl)-1H-indazole-5-carboxamide
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C30H31N5O2
 1
1 IC50 = 1300 nM
CP0058395
2-(ethyl(3-(4-(5-(2-(3-fluorophenylamino)-2-oxoethyl)-1H-pyrazol-3-ylamino)quinazolin-7-yloxy)propyl)amino)ethyl dihydrogen phosphate
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C26H31FN7O6P
 2
1 IC50 = 1400 nM
2 Ki = 1368 nM
CP0018477
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
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C21H16ClF3N4O3
 2
1 IC50 = 3800 nM
2 Kd > 10000 nM
CP0278627
benzyl N-[[4-[3-[[4-(2-pyrrolidin-1-ylethoxy)benzoyl]amino]-1H-pyrazol-5-yl]phenyl]methyl]carbamate
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C31H33N5O4
 1
1 IC50 > 1000 nM
CP0005066
NR9
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C18H13N3OS2
 1
1 IC50 > 10000 nM
CP0030740
1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea
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C29H32N6O4S
 2
1 IC50 > 10000 nM
2 Kd > 10000 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 = 5.8 nM
CP0088050
US9447092, 1
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C22H23Cl2N7
 1
1 Kd = 7.5 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 = 9.3 nM
CP0016677
N-[(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]-N-methylbenzamide
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C35H30N4O4
 2
1 Kd = 19.29 nM
2 Kd = 120 nM
CP0047080
4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-[2-(6-methylpyridin-3-yl)oxyethylamino]pyridine-3-carbonitrile
   Show/Hide
C19H21N7O
 1
1 Km = 28000 nM
Clinical Information about the Protein
Target 1 ( Aurora kinase A (AURKA) )
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 Acute myeloid leukaemia [ICD-11: 2A60]
4 Prostate cancer [ICD-11: 2C82.0]
5 Diabetic complication [ICD-11: 5A2Y]
6 Advanced solid tumour [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 14 Clinical Trial Drugs  14
1 AT9283 Phase 3
Solid tumour/cancer
2 MLN8237 Phase 3
Solid tumour/cancer
3 ABT-348 Phase 2
Haematological malignancy
4 ENMD-2076 Phase 2
Acute myeloid leukaemia
5 PHA-739358 Phase 2
Prostate cancer
6 VX-680 Phase 2
Solid tumour/cancer
7 LY3295668 Phase 1/2
Solid tumour/cancer
8 AMG 900 Phase 1
Solid tumour/cancer
9 CYC116 Phase 1
Solid tumour/cancer
10 MK-5108 Phase 1
Solid tumour/cancer
11 MLN8054 Phase 1
Solid tumour/cancer
12 R763 Phase 1
Haematological malignancy
13 Rosiglitazone + metformin Phase 3
Diabetic complication
14 SNS-314 Phase 1
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 PF-03814735 Discontinued in Phase 1
Advanced solid tumour