General Information of the Protein
Protein ID
PT01042
Protein Name
Serine/threonine-protein kinase PAK 1
Secondarily
Protein Name
Alpha-PAK
p21-activated kinase 1
p65-PAK
Gene Name
PAK1
Sequence
MSNNGLDIQDKPPAPPMRNTSTMIGAGSKDAGTLNHGSKPLPPNPEEKKKKDRFYRSILPGDKTNKKKEKERPEISLPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKSEQKKNPQAVLDVLEFYNSKKTSNSQKYMSFTDKSAEDYNSSNALNVKAVSETPAVPPVSEDEDDDDDDATPPPVIAPRPEHTKSVYTRSVIEPLPVTPTRDVATSPISPTENNTTPPDALTRNTEKQKKKPKMSDEEILEKLRSIVSVGDPKKKYTRFEKIGQGASGTVYTAMDVATGQEVAIKQMNLQQQPKKELIINEILVMRENKNPNIVNYLDSYLVGDELWVVMEYLAGGSLTDVVTETCMDEGQIAAVCRECLQALEFLHSNQVIHRDIKSDNILLGMDGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAYGPKVDIWSLGIMAIEMIEGEPPYLNENPLRALYLIATNGTPELQNPEKLSAIFRDFLNRCLEMDVEKRGSAKELLQHQFLKIAKPLSSLTPLIAAAKEATKNNH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
STE protein kinase group
>
STE protein kinase STE20 family
>
STE protein kinase PAKA subfamily
Function
Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes (PubMed:10551809, PubMed:11896197, PubMed:12876277, PubMed:14585966, PubMed:15611088, PubMed:17726028, PubMed:17989089, PubMed:30290153). Can directly phosphorylate BAD and protects cells against apoptosis (By similarity). Activated by interaction with CDC42 and RAC1 (PubMed:8805275, PubMed:9528787). Functions as a GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway (PubMed:8805275, PubMed:9528787). Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases (By similarity). Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes (PubMed:9395435, PubMed:9032240). Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton (PubMed:15831477). Plays a role in the regulation of insulin secretion in response to elevated glucose levels (PubMed:22669945). Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ) (By similarity). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2 (PubMed:12624090). Phosphorylates MYL9/MLC2 (By similarity). Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2 (PubMed:11733498). Phosphorylates SNAI1 at 'Ser-246' promoting its transcriptional repressor activity by increasing its accumulation in the nucleus (PubMed:15833848). In podocytes, promotes NR3C2 nuclear localization (By similarity). Required for atypical chemokine receptor ACKR2-induced phosphorylation of LIMK1 and cofilin (CFL1) and for the up-regulation of ACKR2 from endosomal compartment to cell membrane, increasing its efficiency in chemokine uptake and degradation (PubMed:23633677). In synapses, seems to mediate the regulation of F-actin cluster formation performed by SHANK3, maybe through CFL1 phosphorylation and inactivation (By similarity). Plays a role in RUFY3-mediated facilitating gastric cancer cells migration and invasion (PubMed:25766321). In response to DNA damage, phosphorylates MORC2 which activates its ATPase activity and facilitates chromatin remodeling (PubMed:23260667). In neurons, plays a crucial role in regulating GABA(A) receptor synaptic stability and hence GABAergic inhibitory synaptic transmission through its role in F-actin stabilization (By similarity). In hippocampal neurons, necessary for the formation of dendritic spines and excitatory synapses; this function is dependent on kinase activity and may be exerted by the regulation of actomyosin contractility through the phosphorylation of myosin II regulatory light chain (MLC) (By similarity). Along with GIT1, positively regulates microtubule nucleation during interphase (PubMed:27012601). Phosphorylates FXR1, promoting its localization to stress granules and activity (PubMed:20417602).
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Uniprot ID
Primary ID:
Q13153

Secondarily ID:
O75561
Q13567
Q32M53
Q32M54
Q86W79
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Ensembl ID
ENSG00000149269
HGNC ID
HGNC:8590
Subcellular Location
Cytoplasm
Cell junction
Focal adhesion
Cell projection
Lamellipodium
Cell membrane
Cell projection
Ruffle membrane
Cell projection
Invadopodium
Nucleus
Nucleoplasm
Chromosome
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
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: CL000504 , EBC-1
Compound ID Compound Name Compound Formula
CP0256326
CHEMBL3770588
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C28H31ClN6O
 1
1
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0156094
6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-8-[[(4S)-3,3-difluoropiperidin-4-yl]methyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C26H25ClF2N6O
 1
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
CP0486462
CHEMBL3769478
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C26H27ClN6O3
 1
1
IC50 = 57 nM
   TI
   LI
   LO
   TS
CP0070883
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H25ClN6O3
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0090236
6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-8-(5,9-dioxa-2-azaspiro[3.5]nonan-7-ylmethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C27H27ClN6O3
 1
1
IC50 = 73 nM
   TI
   LI
   LO
   TS
CP0072137
2-N-[(4-chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-ethylpyrimidine-2,4-diamine
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C20H21ClN8
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0677749
N2-((4-Chloro-1H-benzo[d]imidazol-5-yl)methyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-methylpyrimidine-2,4-diamine
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C19H19ClN8
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0698981
(S)-N2-(1-(1H-Indol-5-yl)ethyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C20H21N7
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0231643
8-[(4-aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-one
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C27H30ClN7O
 1
1
IC50 = 124 nM
   TI
   LI
   LO
   TS
CP0231644
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(piperidin-4-ylmethyl)pyrido[2,3-d]pyrimidin-7-one
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C26H28ClN7O
 1
1
IC50 = 145 nM
   TI
   LI
   LO
   TS
CP0256327
8-(4-aminobutyl)-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-one
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C24H26ClN7O
 1
1
IC50 = 147 nM
   TI
   LI
   LO
   TS
CP0452337
8-[(5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-one
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C25H26ClN7O3
 1
1
IC50 = 148 nM
   TI
   LI
   LO
   TS
CP0098902
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-one
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C28H32ClN7O
 1
1
IC50 = 222 nM
   TI
   LI
   LO
   TS
CP0709895
N2-[(1S)-1-(1H-Benzimidazol-5-yl)ethyl]-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C19H20N8
 1
1
IC50 = 281 nM
   TI
   LI
   LO
   TS
CP0256325
8-[(4-aminocyclohexyl)methyl]-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C26H28ClN7O
 1
1
IC50 = 341 nM
   TI
   LI
   LO
   TS
CP0252383
2-N-[(4-chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C18H17ClN8
 1
1
IC50 = 362 nM
   TI
   LI
   LO
   TS
CP0111952
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)-8-[[(2R)-morpholin-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-one
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C24H24ClN7O2
 1
1
IC50 = 399 nM
   TI
   LI
   LO
   TS
CP0472537
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-[(2-oxopiperidin-4-yl)methyl]pyrido[2,3-d]pyrimidin-7-one
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C26H26ClN7O2
 1
1
IC50 = 813 nM
   TI
   LI
   LO
   TS
CP0256324
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(3-hydroxypropyl)pyrido[2,3-d]pyrimidin-7-one
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C23H23ClN6O2
 1
1
IC50 = 980 nM
   TI
   LI
   LO
   TS
CP0733200
N2-((trans-4-Aminocyclohexyl)methyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C17H25N7
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0065733
2-[[N-[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-5-(hydroxymethyl)-2-methylanilino]methyl]benzonitrile
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C33H36FN7O3S
 1
1 IC50 = 0.33 nM
CP0308873
[3-[[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-[(2-fluorophenyl)methyl]amino]-4-methylphenyl]methanol
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C32H36F2N6O3S
 1
1 IC50 = 0.35 nM
CP0067714
[5-[[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanol
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C27H35FN6O3S
 1
1 IC50 = 0.45 nM
CP0094539
[5-[[2-[3-ethylsulfonyl-4-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]anilino]-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanol
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C28H35FN6O3S
 1
1 IC50 = 0.58 nM
CP0659758
(2-Chlorophenyl)(5-(2-methyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl)methanone
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C24H20ClN3O
 1
1 IC50 = 1 nM
CP0447386
[3-[benzyl-[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]amino]-4-methylphenyl]methanol
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C32H37FN6O3S
 1
1 IC50 = 1.5 nM
CP0155293
[3-[ethyl-[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]amino]-4-methylphenyl]methanol
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C27H35FN6O3S
 1
1 IC50 = 2 nM
CP0308874
[3-[[2-[3-ethylsulfonyl-4-(4-methylpiperazin-1-yl)anilino]-5-fluoropyrimidin-4-yl]-methylamino]-4-methylphenyl]methanol
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C26H33FN6O3S
 1
1 IC50 = 2.1 nM
CP0788333
5-(2-chloro-4-(thiazol-5-yl)phenyl)-3-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4(3H)-one
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C26H27ClN6OS
 1
1 IC50 = 2.8 nM
CP0059523
6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one
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C29H28ClN7OS
 5
1 IC50 = 2.8 nM
2 IC50 = 7.7 nM
3 IC50 <= 10 nM
4 IC50 = 14 nM
5 IC50 = 23 nM
CP0155295
[5-[[2-(3-ethylsulfonyl-5-morpholin-4-ylanilino)-5-fluoropyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanol
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C26H32FN5O4S
 1
1 IC50 = 2.8 nM
CP0551423
[5-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanol
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C25H30FN5O4S
 1
1 IC50 = 3 nM
CP0660192
7-[3-[(2-Chlorophenyl)carbonyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-2-methyl-1,2,3,4-tetrahydroisoquinoline
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C24H20ClN3O
 1
1 IC50 = 4.5 nM
CP0059452
(3S)-3-[[8-chloro-11-(2,2-difluoroethyl)-3-fluoro-5H-benzo[b][1,4]benzodiazepin-6-ylidene]amino]-N-propan-2-ylpyrrolidine-1-carboxamide
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C23H25ClF3N5O
 2
1 IC50 = 6 nM
2 Kd = 7 nM
CP0155297
[3-[[5-fluoro-2-[4-(4-methylpiperazin-1-yl)-3-methylsulfonylanilino]pyrimidin-4-yl]-methylamino]-4-methylphenyl]methanol
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C25H31FN6O3S
 1
1 IC50 = 8.7 nM
CP0181332
[4-chloro-3-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]phenyl]methanol
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C23H25ClFN5O4S
 1
1 IC50 = 9.6 nM
CP0034466
6-[2-chloro-4-(3-methyl-2-oxopyridin-1-yl)phenyl]-N-(pyridin-4-ylmethyl)-1H-indazole-3-carboxamide
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C26H20ClN5O2
 1
1 IC50 = 9.8 nM
CP0098902
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-one
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C28H32ClN7O
 2
1 IC50 <= 10 nM
2 Ki = 22 nM
CP0028071
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide
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C25H30N8OS
 6
1 IC50 = 13.7 nM
2 IC50 = 14 nM
3 IC50 = 36 nM
4 IC50 = 39 nM
5 Ki = 15 nM
6 Ki = 39 nM
CP0067715
[3-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-4-methylphenyl]methanol
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C24H28FN5O4S
 1
1 IC50 = 14 nM
CP0677767
(2-Chlorophenyl)-[5-[1-(4-piperidyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-3-yl]methanone
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C22H20ClN5O
 1
1 IC50 = 18 nM
CP0447394
[5-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]-2-methylphenyl]methanol
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C24H28FN5O4S
 1
1 IC50 = 19 nM
CP0677770
(2-Chlorophenyl)-[5-(2-methylisoindolin-5-yl)-1H-pyrrolo[2,3-b]pyridin-3-yl]methanone
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C23H18ClN3O
 1
1 IC50 = 33 nM
CP0065732
[5-[[5-fluoro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-methylamino]-2,4-dimethylphenyl]methanol
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C25H31FN6O
 1
1 IC50 = 33 nM
CP0566823
[3-[[5-fluoro-2-(3-methylsulfonyl-5-morpholin-4-ylanilino)pyrimidin-4-yl]-methylamino]phenyl]methanol
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C23H26FN5O4S
 1
1 IC50 = 45 nM
CP0842155
(R/S)-2-(3-(5-bromo-2-(4-(3,4-dimethylpiperazin-1-yl)-3-methoxyphenylamino)pyrimidin-4-yl)phenyl)acetonitrile
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C25H27BrN6O
 1
1 IC50 = 61 nM
CP0075213
2-[3-[5-bromo-2-[4-[(3S)-3,4-dimethylpiperazin-1-yl]-3-methoxyanilino]pyrimidin-4-yl]phenyl]acetonitrile
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C25H27BrN6O
 1
1 IC50 = 65 nM
CP0075212
2-[3-[5-bromo-2-[4-[(3R)-3,4-dimethylpiperazin-1-yl]-3-methoxyanilino]pyrimidin-4-yl]phenyl]acetonitrile
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C25H27BrN6O
 1
1 IC50 = 72 nM
CP0318706
2-[3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-5-fluorophenyl]acetonitrile
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C24H24ClFN6O
 1
1 IC50 = 98 nM
CP0207621
(4-methyl-3-(methyl(2-(3-(methylsulfonyl)-5-morpholinophenylamino)pyrimidin-4-yl)amino)phenyl)methanol
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C24H29N5O4S
 1
1 IC50 = 100 nM
CP0075218
2-[3-chloro-5-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C24H24Cl2N6O
 1
1 IC50 = 103 nM
CP0018775
2-[3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C24H25ClN6O
 1
1 IC50 = 110 nM
CP0257999
2-[3-[5-chloro-2-[4-(3,4-dimethylpiperazin-1-yl)-3-methoxyanilino]pyrimidin-4-yl]phenyl]acetonitrile
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C25H27ClN6O
 1
1 IC50 = 126 nM
CP0563708
5-fluoro-4-N-[5-(methoxymethyl)-2-methylphenyl]-4-N-methyl-2-N-(3-methylsulfonyl-5-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
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C25H30FN5O4S
 1
1 IC50 = 189 nM
CP0221823
3-chloro-5-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]benzonitrile
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C23H22Cl2N6O
 1
1 IC50 = 227 nM
CP0761670
1-[6-[3-(2-Chlorobenzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-3,4-dihydro-1H-isoquinolin-2-yl]ethanone
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C25H20ClN3O2
 1
1 IC50 = 270 nM
CP0075214
ethyl 5-[[5-chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-2-(4-methylpiperazin-1-yl)benzoate
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C26H27ClN6O2
 1
1 IC50 = 289 nM
CP0258399
3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-5-methoxybenzonitrile
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C24H25ClN6O2
 1
1 IC50 = 487 nM
CP0075216
2-[3-[5-chloro-2-[3-fluoro-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C23H22ClFN6
 1
1 IC50 = 548 nM
CP0258397
2-[3-[5-chloro-2-[3-(5-methyl-1,3-oxazol-2-yl)-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C27H26ClN7O
 1
1 IC50 = 636 nM
CP0075215
2-[3-[5-chloro-2-[3-hydroxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C23H23ClN6O
 1
1 IC50 = 674 nM
CP0258398
5-[[5-chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-2-(4-methylpiperazin-1-yl)benzonitrile
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C24H22ClN7
 1
1 IC50 = 780 nM
CP0287070
2-[3-[5-chloro-2-[3-ethoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C25H27ClN6O
 1
1 IC50 = 957 nM
CP0241043
2-[3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]-2-methylpropanenitrile
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C26H29ClN6O
 1
1 IC50 = 985 nM
CP0285798
2-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)-3-(1,3-oxazol-2-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C26H24ClN7O
 1
1 IC50 = 1420 nM
CP0223817
3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]-N-(cyanomethyl)benzamide
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C25H26ClN7O2
 1
1 IC50 = 2140 nM
CP0042893
ethyl 3-[5-chloro-2-[3-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]benzoate
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C25H28ClN5O3
 1
1 IC50 = 2680 nM
CP0223815
2-[3-[5-chloro-2-[3-(2-methoxyethoxy)-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]phenyl]acetonitrile
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C26H29ClN6O2
 1
1 IC50 = 2880 nM
CP0176110
5-[[5-chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-N,N-diethyl-2-(4-methylpiperazin-1-yl)benzamide
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C28H32ClN7O
 1
1 IC50 = 4010 nM
CP0322736
6-(2-chlorophenyl)-N-methyl-1H-indazole-3-carboxamide
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C15H12ClN3O
 1
1 IC50 = 5000 nM
CP0243914
5-[[5-chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-N-methyl-2-(4-methylpiperazin-1-yl)benzamide
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C25H26ClN7O
 1
1 IC50 = 6550 nM
CP0176111
5-[[5-chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-2-(4-methylpiperazin-1-yl)benzoic acid
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C24H23ClN6O2
 1
1 IC50 = 11300 nM
CP0231643
CHEMBL3770909
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C27H30ClN7O
 1
1 Ki = 1.9 nM
CP0486462
CHEMBL3769478
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C26H27ClN6O3
 1
1 Ki = 1.9 nM
CP0256326
CHEMBL3770588
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C28H31ClN6O
 1
1 Ki = 2.1 nM
CP0070883
CHEMBL3770443
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C25H25ClN6O3
 1
1 Ki = 3.7 nM
CP0677749
N2-((4-Chloro-1H-benzo[d]imidazol-5-yl)methyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-methylpyrimidine-2,4-diamine
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C19H19ClN8
 2
1 Ki = 4 nM
2 Ki = 5 nM
CP0090236
6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-8-(5,9-dioxa-2-azaspiro[3.5]nonan-7-ylmethyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C27H27ClN6O3
 1
1 Ki = 4.3 nM
CP0072137
2-N-[(4-chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-N-ethylpyrimidine-2,4-diamine
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C20H21ClN8
 1
1 Ki = 5 nM
CP0252383
2-N-[(4-chloro-1H-benzimidazol-5-yl)methyl]-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C18H17ClN8
 1
1 Ki = 5 nM
CP0231644
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(piperidin-4-ylmethyl)pyrido[2,3-d]pyrimidin-7-one
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C26H28ClN7O
 1
1 Ki = 6 nM
CP0256327
8-(4-aminobutyl)-6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)pyrido[2,3-d]pyrimidin-7-one
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C24H26ClN7O
 1
1 Ki = 6.1 nM
CP0256325
CHEMBL3769456
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C26H28ClN7O
 1
1 Ki = 7.4 nM
CP0156094
6-[2-chloro-4-(6-methylpyridin-2-yl)phenyl]-8-[[(4S)-3,3-difluoropiperidin-4-yl]methyl]-2-(methylamino)pyrido[2,3-d]pyrimidin-7-one
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C26H25ClF2N6O
 1
1 Ki = 7.9 nM
CP0452337
CHEMBL3770295
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C25H26ClN7O3
 1
1 Ki = 8 nM
CP0709895
N2-[(1S)-1-(1H-Benzimidazol-5-yl)ethyl]-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C19H20N8
 1
1 Ki = 12 nM
CP0659882
(3R)-3-[3-[[2-[(4-chloro-3H-benzimidazol-5-yl)methyl-methyl-amino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methyl-pyrrolidin-2-one
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C21H22ClN9O
 1
1 Ki = 18 nM
CP0111952
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(methylamino)-8-[[(2R)-morpholin-2-yl]methyl]pyrido[2,3-d]pyrimidin-7-one
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C24H24ClN7O2
 1
1 Ki = 19 nM
CP0733200
N2-((trans-4-Aminocyclohexyl)methyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C17H25N7
 1
1 Ki = 26 nM
CP0698981
(S)-N2-(1-(1H-Indol-5-yl)ethyl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
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C20H21N7
 1
1 Ki = 31 nM
CP0717532
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-methyl-amino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methyl-pyrrolidin-2-one
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C20H30N8O
 1
1 Ki = 37 nM
CP0642833
(3R)-3-[3-[[2-[(4-Aminocyclohexyl)methyl-ethyl-amino]pyrimidin-4-yl]amino]-1H-pyrazol-5-yl]-1-methyl-pyrrolidin-2-one
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C21H32N8O
 1
1 Ki = 49 nM
CP0256324
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-(3-hydroxypropyl)pyrido[2,3-d]pyrimidin-7-one
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C23H23ClN6O2
 1
1 Ki = 64 nM
CP0472537
6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-2-(ethylamino)-8-[(2-oxopiperidin-4-yl)methyl]pyrido[2,3-d]pyrimidin-7-one
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C26H26ClN7O2
 1
1 Ki = 66 nM
Clinical Information about the Protein
Target 1 ( PAK-1 protein kinase (PAK1) )
Target Type Literature-reported Target