General Information of the Protein
Protein ID
PT01141
Protein Name
Focal adhesion kinase 1
Secondarily
Protein Name
Focal adhesion kinase-related nonkinase
Protein phosphatase 1 regulatory subunit 71
Protein-tyrosine kinase 2
p125FAK
pp125FAK
Gene Name
PTK2
Secondarily
Gene Name
FAK
FAK1
Sequence
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKIAGAPEPLTVTAPSLTIAENMADLIDGYCRLVNGTSQSFIIRPQKEGERALPSIPKLANSEKQGMRTHAVSVSETDDYAEIIDEEDTYTMPSTRDYEIQRERIELGRCIGEGQFGDVHQGIYMSPENPALAVAIKTCKNCTSDSVREKFLQEALTMRQFDHPHIVKLIGVITENPVWIIMELCTLGELRSFLQVRKYSLDLASLILYAYQLSTALAYLESKRFVHRDIAARNVLVSSNDCVKLGDFGLSRYMEDSTYYKASKGKLPIKWMAPESINFRRFTSASDVWMFGVCMWEILMHGVKPFQGVKNNDVIGRIENGERLPMPPNCPPTLYSLMTKCWAYDPSRRPRFTELKAQLSTILEEEKAQQEERMRMESRRQATVSWDSGGSDEAPPKPSRPGYPSPRSSEGFYPSPQHMVQTNHYQVSGYPGSHGITAMAGSIYPGQASLLDQTDSWNHRPQEIAMWQPNVEDSTVLDLRGIGQVLPTHLMEERLIRQQQEMEEDQRWLEKEERFLKPDVRLSRGSIDREDGSLQGPIGNQHIYQPVGKPDPAAPPKKPPRPGAPGHLGSLASLSSPADSYNEGVKLQPQEISPPPTANLDRSNDKVYENVTGLVKAVIEMSSKIQPAPPEEYVPMVKEVGLALRTLLATVDETIPLLPASTHREIEMAQKLLNSDLGELINKMKLAQQYVMTSLQQEYKKQMLTAAHALAVDAKNLLDVIDQARLKMLGQTRPH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Fak family
Function
Non-receptor protein-tyrosine kinase that plays an essential role in regulating cell migration, adhesion, spreading, reorganization of the actin cytoskeleton, formation and disassembly of focal adhesions and cell protrusions, cell cycle progression, cell proliferation and apoptosis. Required for early embryonic development and placenta development. Required for embryonic angiogenesis, normal cardiomyocyte migration and proliferation, and normal heart development. Regulates axon growth and neuronal cell migration, axon branching and synapse formation; required for normal development of the nervous system. Plays a role in osteogenesis and differentiation of osteoblasts. Functions in integrin signal transduction, but also in signaling downstream of numerous growth factor receptors, G-protein coupled receptors (GPCR), EPHA2, netrin receptors and LDL receptors. Forms multisubunit signaling complexes with SRC and SRC family members upon activation; this leads to the phosphorylation of additional tyrosine residues, creating binding sites for scaffold proteins, effectors and substrates. Regulates numerous signaling pathways. Promotes activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascade. Promotes activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling cascade. Promotes localized and transient activation of guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs), and thereby modulates the activity of Rho family GTPases. Signaling via CAS family members mediates activation of RAC1. Phosphorylates NEDD9 following integrin stimulation (PubMed:9360983). Recruits the ubiquitin ligase MDM2 to P53/TP53 in the nucleus, and thereby regulates P53/TP53 activity, P53/TP53 ubiquitination and proteasomal degradation. Phosphorylates SRC; this increases SRC kinase activity. Phosphorylates ACTN1, ARHGEF7, GRB7, RET and WASL. Promotes phosphorylation of PXN and STAT1; most likely PXN and STAT1 are phosphorylated by a SRC family kinase that is recruited to autophosphorylated PTK2/FAK1, rather than by PTK2/FAK1 itself. Promotes phosphorylation of BCAR1; GIT2 and SHC1; this requires both SRC and PTK2/FAK1. Promotes phosphorylation of BMX and PIK3R1. Isoform 6 (FRNK) does not contain a kinase domain and inhibits PTK2/FAK1 phosphorylation and signaling. Its enhanced expression can attenuate the nuclear accumulation of LPXN and limit its ability to enhance serum response factor (SRF)-dependent gene transcription.
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Uniprot ID
Primary ID:
Q05397

Secondarily ID:
B4E2N6
F5H4S4
J3QT16
Q14291
Q8IYN9
Q9UD85
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Ensembl ID
ENSG00000169398
HGNC ID
HGNC:9611
Subcellular Location
Cell junction
Focal adhesion
Cell membrane
Cytoplasm
Perinuclear region
Cytoplasm
Cell cortex
Cytoplasm
Cytoskeleton
Cytoplasm
Cytoskeleton
Microtubule organizing center
Centrosome
Nucleus
Cytoplasm
Cytoskeleton
Cilium basal body
Cytoplasm
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: CL000928 , 293GT
Compound ID Compound Name Compound Formula
CP0016998
2-[4-[4-[[5-chloro-7-[2-[methyl(methylsulfonyl)amino]phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C27H30ClN7O3S
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0392582
2-[4-[4-[[7-[2-[methyl(methylsulfonyl)amino]phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C27H31N7O3S
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0474017
2-[4-[4-[[7-[3-(methanesulfonamido)phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H29N7O3S
 1
1
IC50 = 660 nM
   TI
   LI
   LO
   TS
CP0387525
2-[4-[4-[[7-(2-methoxyphenyl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H28N6O2
 1
1
IC50 = 690 nM
   TI
   LI
   LO
   TS
CP0391780
2-[4-[4-[[7-[2-[methyl(methylsulfonyl)amino]pyridin-3-yl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H30N8O3S
 1
1
IC50 = 750 nM
   TI
   LI
   LO
   TS
CP0456832
2-[4-[4-[[7-(3-methylsulfonylphenyl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H28N6O3S
 1
1
IC50 = 1010 nM
   TI
   LI
   LO
   TS
CP0509092
2-[4-[4-[[7-(6-methoxypyridin-3-yl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C25H27N7O2
 1
1
IC50 = 1190 nM
   TI
   LI
   LO
   TS
CP0392584
2-[4-[4-[[5-methyl-7-[2-[methyl(methylsulfonyl)amino]phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C28H33N7O3S
 1
1
IC50 = 1230 nM
   TI
   LI
   LO
   TS
CP0489047
2-[4-[4-[[7-[3-(tert-butylsulfamoyl)phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C29H35N7O3S
 1
1
IC50 = 1340 nM
   TI
   LI
   LO
   TS
CP0392583
2-[4-[4-[[7-[3-(hydroxymethyl)phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H28N6O2
 1
1
IC50 = 1390 nM
   TI
   LI
   LO
   TS
CP0390801
2-[4-[4-[[7-(4-methylsulfonylphenyl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C26H28N6O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0454945
2-[4-[4-[[7-(3-methoxypyridin-2-yl)pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C25H27N7O2
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0454946
2-[4-[4-[[7-[3-[methyl(methylsulfonyl)amino]phenyl]pyrrolo[2,1-f][1,2,4]triazin-2-yl]amino]phenyl]piperidin-1-yl]acetamide
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C27H31N7O3S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
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
 13
1 EC50 = 24263.72873 nM
2 IC50 = 9.12 nM
3 IC50 = 11 nM
4 IC50 = 13 nM
5 IC50 = 13.2 nM
6 IC50 = 17.15 nM
7 IC50 = 20 nM
8 IC50 = 55 nM
9 IC50 = 80 nM
10 IC50 = 500 nM
11 IC50 = 3120 nM
12 Kd = 64 nM
13 Kd = 68 nM
CP0029290
N-methyl-4-({4-[({3- [methyl(methylsulfonyl)amino]pyrazin-2- yl}methyl)amino]-5- (trifluoromethyl)pyrimidin-2- yl}amino)benzamide (317)
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C20H21F3N8O3S
 8
1 IC50 = 0.2 nM
2 IC50 < 0.5 nM
3 IC50 = 0.6 nM
4 IC50 = 0.63 nM
5 IC50 < 1 nM
6 IC50 = 1.16 nM
7 IC50 = 3.9 nM
8 IC50 ~ 0.2 nM
CP0322343
2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-N-methoxybenzamide
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C20H23ClN6O2
 1
1 IC50 = 0.4 nM
CP0140704
2-[[5-chloro-2-[4-[[[3,4-dioxo-2-[2-(prop-2-enoylamino)ethylamino]cyclobuten-1-yl]amino]methyl]anilino]pyrimidin-4-yl]amino]-N-methylbenzamide
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C28H27ClN8O4
 1
1 IC50 = 0.6 nM
CP0153321
N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]methanesulfonamide
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C21H20F3N7O3S
 2
1 IC50 = 1 nM
2 IC50 = 1.5 nM
CP0226420
US9012461, 3
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C26H29F3N6O
 2
1 IC50 = 1.1 nM
2 Kd = 0.91 nM
CP0211896
US9012461, 11
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C26H28F3N5O
 2
1 IC50 = 2.5 nM
2 Kd = 0.61 nM
CP0468039
US9012461, 24
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C28H30F3N5O2
 2
1 IC50 = 3.9 nM
2 Kd = 0.77 nM
CP0019886
6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one
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C22H20F3N5O3S
 1
1 IC50 = 4 nM
CP0117454
2-(5-chloro-2-(2-methoxy-4-morpholinophenylamino)pyrimidin-4-ylamino)-N-methylbenzamide
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C23H25ClN6O3
 5
1 IC50 = 4.502 nM
2 IC50 = 5.5 nM
3 IC50 = 7 nM
4 IC50 = 36 nM
5 IC50 = 5200 nM
CP0262466
US9012461, 8
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C26H28F3N5O
 2
1 IC50 = 4.8 nM
2 Kd = 1 nM
CP0334858
US9012461, 20
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C26H29F3N6O
 2
1 IC50 = 5 nM
2 Kd = 0.63 nM
CP0501518
US9012461, 30
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C25H28F3N7O
 2
1 IC50 = 7 nM
2 Kd = 5.7 nM
CP0251119
US9012461, 16
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C27H30F3N5O
 2
1 IC50 = 11 nM
2 Kd = 1.3 nM
CP0251702
US9012461, 12
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C27H30F3N5O
 2
1 IC50 = 12 nM
2 Kd = 0.92 nM
CP0251706
US9012461, 31
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C28H32F3N5O
 2
1 IC50 = 12 nM
2 Kd = 1 nM
CP0334860
US9012461, 25
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C26H29F3N6O
 2
1 IC50 = 14 nM
2 Kd = 1.1 nM
CP0332519
US9012461, 22
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C25H26F3N5O2
 2
1 IC50 = 15 nM
2 Kd = 0.99 nM
CP0231380
US9012461, 36
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C27H31F3N6O
 2
1 IC50 = 16 nM
2 Kd = 0.48 nM
CP0325784
US9012461, 33
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C26H29F3N6O
 2
1 IC50 = 16 nM
2 Kd = 5.6 nM
CP0569107
US9012461, 21
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C24H24F3N5O
 2
1 IC50 = 25 nM
2 Kd = 0.44 nM
CP0519009
US9012461, 17
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C26H29F3N6O
 2
1 IC50 = 31 nM
2 Kd = 3.5 nM
CP0186869
N-[3-[[[2-(4-fluorophenyl)-5-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C22H19F4N5O2S
 2
1 IC50 = 37 nM
2 Kd = 24 nM
CP0248673
2-[[5-cyano-2-(4-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]-N-methylbenzamide
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C22H16FN5O
 2
1 IC50 = 37 nM
2 Kd = 40 nM
CP0131892
N-methyl-2-[[2-(4-morpholin-4-ylphenyl)-5-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]benzamide
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C26H24F3N5O2
 2
1 IC50 = 45 nM
2 Kd = 35 nM
CP0208534
N-methyl-2-[[2-(6-morpholin-4-ylpyridin-3-yl)-5-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]benzamide
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C25H23F3N6O2
 2
1 IC50 = 45 nM
2 Kd = 9 nM
CP0208523
2-[[2-(4-fluorophenyl)-5-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]-N-methylbenzamide
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C22H16F4N4O
 1
1 IC50 = 51 nM
CP0131893
N-methyl-2-[[2-pyridin-3-yl-5-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]benzamide
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C21H16F3N5O
 2
1 IC50 = 57 nM
2 Kd = 12 nM
CP0214560
N-[3-[[[2-(4-fluorophenyl)-6-(trifluoromethyl)-1H-imidazo[4,5-b]pyridin-7-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C21H18F4N6O2S
 2
1 IC50 = 130 nM
2 Kd = 33 nM
CP0089290
(1S,2S,3R,4R)-3-[[5-chloro-2-[[(7S)-4-methoxy-7-morpholin-4-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
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C28H35ClN6O3
 1
1 IC50 = 133 nM
CP0156809
2-[[6-bromo-2-(4-fluorophenyl)-1H-imidazo[4,5-b]pyridin-7-yl]amino]-N-methylbenzamide
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C20H15BrFN5O
 2
1 IC50 = 170 nM
2 Kd = 127 nM
CP0156804
N-[3-[[[5-cyano-2-(4-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C22H19FN6O2S
 2
1 IC50 = 177 nM
2 Kd = 603 nM
CP0131889
N-[3-[[(5-cyano-2-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C22H20N6O2S
 2
1 IC50 = 195 nM
2 Kd = 44 nM
CP0772886
(Z)-2(2)-fluoro-31,5-dimethyl-6-oxo-13-(trifluoromethyl)-1(1)H,2(1)H,3(1)H-5-aza-2(3,5)-pyrrolo[2,3-b]pyridina-1(4,1),3(4,3)-dipyrazolacyclononaphane-35-carbonitrile
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C22H18F4N8O
 1
1 IC50 = 210 nM
CP0186868
N-[3-[[[5-cyano-2-(2-methylpyridin-4-yl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C22H21N7O2S
 2
1 IC50 = 220 nM
2 Kd = 24 nM
CP0031656
1-[4-(6-aminopurin-9-yl)phenyl]-3-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]urea
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C26H27N9O
 2
1 IC50 = 266 nM
2 Kd = 111 nM
CP0319410
N-[(4-fluorophenyl)methyl]-1,5-dimethyl-4,4-dioxopyrazolo[4,3-c][2,1]benzothiazin-8-amine
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C18H17FN4O2S
 1
1 IC50 = 320 nM
CP0185378
N-[(4-tert-butylphenyl)methyl]-1,5-dimethyl-4,4-dioxopyrazolo[4,3-c][2,1]benzothiazin-8-amine
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C22H26N4O2S
 2
1 IC50 = 640 nM
2 IC50 = 2200 nM
CP0156807
N-[3-[[[2-(4-bromophenyl)-6-(trifluoromethyl)-1H-imidazo[4,5-b]pyridin-7-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C21H18BrF3N6O2S
 2
1 IC50 = 700 nM
2 Kd = 189 nM
CP0239611
N-[3-[[[2-(4-fluorophenyl)-5-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C22H22FN5O2S
 2
1 IC50 = 910 nM
2 Kd = 554 nM
CP0247562
N-[(4-bromophenyl)methyl]-1,5-dimethyl-4,4-dioxopyrazolo[4,3-c][2,1]benzothiazin-8-amine
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C18H17BrN4O2S
 1
1 IC50 = 1400 nM
CP0131887
N-[3-[[(5-cyano-1H-pyrrolo[2,3-b]pyridin-4-yl)amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C16H16N6O2S
 2
1 IC50 = 2400 nM
2 Kd = 147 nM
CP0315915
N-(4-fluorophenyl)-1,5-dimethyl-4,4-dioxopyrazolo[4,3-c][2,1]benzothiazin-8-amine
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C17H15FN4O2S
 1
1 IC50 = 4300 nM
CP0156805
N-[3-[[[6-bromo-2-(4-fluorophenyl)-1H-imidazo[4,5-b]pyridin-7-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C20H18BrFN6O2S
 2
1 IC50 = 4500 nM
2 Kd = 335 nM
CP0186865
N-[3-[[[2-(4-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
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C21H20FN5O2S
 2
1 IC50 = 4800 nM
2 Kd = 6380 nM
CP0026310
1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-(4-pyridin-3-ylphenyl)urea
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C26H27N5O
 2
1 IC50 = 7000 nM
2 Kd = 770 nM
CP0026311
1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(4-methylimidazol-1-yl)phenyl]urea
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C25H28N6O
 2
1 IC50 = 7700 nM
2 Kd = 1040 nM
CP0072404
1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(4,5-dichloroimidazol-1-yl)phenyl]urea
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C24H24Cl2N6O
 2
1 IC50 = 8400 nM
2 Kd = 4590 nM
CP0214555
N-methyl-N-[3-[[(5-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)amino]methyl]pyridin-2-yl]methanesulfonamide
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C16H19N5O2S
 2
1 IC50 = 8800 nM
2 Kd = 1700 nM
CP0072409
1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-(4-imidazol-1-ylphenyl)urea
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C24H26N6O
 2
1 IC50 = 9100 nM
2 Kd = 1530 nM
Clinical Information about the Protein
Target 1 ( Focal adhesion kinase 1 (FAK) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
2 Ovarian cancer [ICD-11: 2C73]
Clinical Trial Drug(s) 5 Clinical Trial Drugs  5
1 CEP-37440 Phase 1
Solid tumour/cancer
2 GSK-2256098 Phase 1
Solid tumour/cancer
3 PF-562271 Phase 1
Solid tumour/cancer
4 VS-6063 Phase 2
Ovarian cancer
5 VS-4718 Phase 1
Solid tumour/cancer