General Information of the Protein
Protein ID
PT01098
Protein Name
Protein-tyrosine kinase 2-beta
Secondarily
Protein Name
Calcium-dependent tyrosine kinase
Calcium-regulated non-receptor proline-rich tyrosine kinase
Cell adhesion kinase beta
Focal adhesion kinase 2
Proline-rich tyrosine kinase 2
Related adhesion focal tyrosine kinase
Gene Name
PTK2B
Secondarily
Gene Name
FAK2
PYK2
RAFTK
Sequence
MSGVSEPLSRVKLGTLRRPEGPAEPMVVVPVDVEKEDVRILKVCFYSNSFNPGKNFKLVKCTVQTEIREIITSILLSGRIGPNIRLAECYGLRLKHMKSDEIHWLHPQMTVGEVQDKYECLHVEAEWRYDLQIRYLPEDFMESLKEDRTTLLYFYQQLRNDYMQRYASKVSEGMALQLGCLELRRFFKDMPHNALDKKSNFELLEKEVGLDLFFPKQMQENLKPKQFRKMIQQTFQQYASLREEECVMKFFNTLAGFANIDQETYRCELIQGWNITVDLVIGPKGIRQLTSQDAKPTCLAEFKQIRSIRCLPLEEGQAVLQLGIEGAPQALSIKTSSLAEAENMADLIDGYCRLQGEHQGSLIIHPRKDGEKRNSLPQIPMLNLEARRSHLSESCSIESDIYAEIPDETLRRPGGPQYGIAREDVVLNRILGEGFFGEVYEGVYTNHKGEKINVAVKTCKKDCTLDNKEKFMSEAVIMKNLDHPHIVKLIGIIEEEPTWIIMELYPYGELGHYLERNKNSLKVLTLVLYSLQICKAMAYLESINCVHRDIAVRNILVASPECVKLGDFGLSRYIEDEDYYKASVTRLPIKWMSPESINFRRFTTASDVWMFAVCMWEILSFGKQPFFWLENKDVIGVLEKGDRLPKPDLCPPVLYTLMTRCWDYDPSDRPRFTELVCSLSDVYQMEKDIAMEQERNARYRTPKILEPTAFQEPPPKPSRPKYRPPPQTNLLAPKLQFQVPEGLCASSPTLTSPMEYPSPVNSLHTPPLHRHNVFKRHSMREEDFIQPSSREEAQQLWEAEKVKMRQILDKQQKQMVEDYQWLRQEEKSLDPMVYMNDKSPLTPEKEVGYLEFTGPPQKPPRLGAQSIQPTANLDRTDDLVYLNVMELVRAVLELKNELCQLPPEGYVVVVKNVGLTLRKLIGSVDDLLPSLPSSSRTEIEGTQKLLNKDLAELINKMRLAQQNAVTSLSEECKRQMLTASHTLAVDAKNLLDAVDQAKVLANLAHPPAE
    Show/Hide
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 regulates reorganization of the actin cytoskeleton, cell polarization, cell migration, adhesion, spreading and bone remodeling. Plays a role in the regulation of the humoral immune response, and is required for normal levels of marginal B-cells in the spleen and normal migration of splenic B-cells. Required for normal macrophage polarization and migration towards sites of inflammation. Regulates cytoskeleton rearrangement and cell spreading in T-cells, and contributes to the regulation of T-cell responses. Promotes osteoclastic bone resorption; this requires both PTK2B/PYK2 and SRC. May inhibit differentiation and activity of osteoprogenitor cells. Functions in signaling downstream of integrin and collagen receptors, immune receptors, G-protein coupled receptors (GPCR), cytokine, chemokine and growth factor receptors, and mediates responses to cellular stress. 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 of the AKT1 signaling cascade. Promotes activation of NOS3. Regulates production of the cellular messenger cGMP. Promotes activation of the MAP kinase signaling cascade, including activation of MAPK1/ERK2, MAPK3/ERK1 and MAPK8/JNK1. Promotes activation of Rho family GTPases, such as RHOA and RAC1. Recruits the ubiquitin ligase MDM2 to P53/TP53 in the nucleus, and thereby regulates P53/TP53 activity, P53/TP53 ubiquitination and proteasomal degradation. Acts as a scaffold, binding to both PDPK1 and SRC, thereby allowing SRC to phosphorylate PDPK1 at 'Tyr-9, 'Tyr-373', and 'Tyr-376'. Promotes phosphorylation of NMDA receptors by SRC family members, and thereby contributes to the regulation of NMDA receptor ion channel activity and intracellular Ca(2+) levels. May also regulate potassium ion transport by phosphorylation of potassium channel subunits. Phosphorylates SRC; this increases SRC kinase activity. Phosphorylates ASAP1, NPHP1, KCNA2 and SHC1. Promotes phosphorylation of ASAP2, RHOU and PXN; this requires both SRC and PTK2/PYK2.
    Show/Hide
Uniprot ID
Primary ID:
Q14289

Secondarily ID:
D3DST0
Q13475
Q14290
Q16709
Q6PID4
    Show/Hide
Ensembl ID
ENSG00000120899
HGNC ID
HGNC:9612
Subcellular Location
Cytoplasm
Cytoplasm
Perinuclear region
Cell membrane
Cell junction
Focal adhesion
Cell projection
Lamellipodium
Cytoplasm
Cell cortex
Nucleus
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: CL000012 , Sf21
Compound ID Compound Name Compound Formula
CP0508188
16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,14,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(23),3,5,7(25),10(15),11,13,20(24),21-nonaene
   Show/Hide
C21H21F3N6O2S
 1
1
IC50 = 0.67 nM
   TI
   LI
   LO
   TS
CP0532758
4-[(18E)-16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,14,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(24),3,5,7(25),10(15),11,13,18,20,22-decaen-21-yl]morpholine
   Show/Hide
C25H26F3N7O3S
 1
1
IC50 = 0.84 nM
   TI
   LI
   LO
   TS
CP0508490
16-methylsulfonyl-26-(trifluoromethyl)-2,10,16,24,28,29-hexazapentacyclo[23.3.1.13,7.06,10.017,22]triaconta-1(28),3(30),4,6,17,19,21,25(29),26-nonaen-11-one
   Show/Hide
C26H27F3N6O3S
 1
1
IC50 = 0.9 nM
   TI
   LI
   LO
   TS
CP0508489
4-[16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,14,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(24),3,5,7(25),10(15),11,13,20,22-nonaen-21-yl]morpholine
   Show/Hide
C25H28F3N7O3S
 1
1
IC50 = 1.31 nM
   TI
   LI
   LO
   TS
CP0516060
24-methyl-16-methylsulfonyl-26-(trifluoromethyl)-2,10,16,24,28,29-hexazapentacyclo[23.3.1.13,7.06,10.017,22]triaconta-1(28),3(30),4,6,17,19,21,25(29),26-nonaen-11-one
   Show/Hide
C27H29F3N6O3S
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
   TS
CP0408956
4-[(18E)-8-methyl-16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,14,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(24),3,5,7(25),10(15),11,13,18,20,22-decaen-21-yl]morpholine
   Show/Hide
C26H28F3N7O3S
 1
1
IC50 = 1.55 nM
   TI
   LI
   LO
   TS
CP0408955
16-ethylsulfonyl-26-(trifluoromethyl)-2,10,16,24,28,29-hexazapentacyclo[23.3.1.13,7.06,10.017,22]triaconta-1(28),3(30),4,6,17,19,21,25(29),26-nonaen-11-one
   Show/Hide
C27H29F3N6O3S
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0511808
(18E)-16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,14,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(23),3,5,7(25),10(15),11,13,18,20(24),21-decaene
   Show/Hide
C21H19F3N6O2S
 1
1
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0377487
4-[(18E)-8-methyl-16-methylsulfonyl-6-(trifluoromethyl)-2,4,8,13,16,25-hexazatetracyclo[18.3.1.13,7.010,15]pentacosa-1(24),3,5,7(25),10(15),11,13,18,20,22-decaen-21-yl]morpholine
   Show/Hide
C26H28F3N7O3S
 1
1
IC50 = 2.7 nM
   TI
   LI
   LO
   TS
CP0446131
16-methylsulfonyl-26-(trifluoromethyl)-2,10,16,18,24,28,29-heptazapentacyclo[23.3.1.13,7.06,10.017,22]triaconta-1(28),3(30),4,6,17(22),18,20,25(29),26-nonaen-11-one
   Show/Hide
C25H26F3N7O3S
 1
1
IC50 = 3.1 nM
   TI
   LI
   LO
   TS
CP0539694
16,16-dioxo-26-(trifluoromethyl)-16lambda6-thia-2,10,15,18,24,28,29-heptazapentacyclo[23.3.1.13,7.06,10.017,22]triaconta-1(28),3(30),4,6,17(22),18,20,25(29),26-nonaen-11-one
   Show/Hide
C23H22F3N7O3S
 1
1
IC50 = 3.5 nM
   TI
   LI
   LO
   TS
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
   Show/Hide
C21H20F3N7O3S
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0451767
N-[3-[[[2-(3-bromo-4-morpholin-4-ylanilino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]-N-prop-2-enylmethanesulfonamide
   Show/Hide
C25H27BrF3N7O3S
 1
1
IC50 = 19.5 nM
   TI
   LI
   LO
   TS
CP0377488
18-methylsulfonyl-28-(trifluoromethyl)-2,10,18,20,26,30,31-heptazahexacyclo[25.3.1.13,7.112,16.06,10.019,24]tritriaconta-1(30),3(33),4,6,12,14,16(32),19(24),20,22,27(31),28-dodecaen-11-one
   Show/Hide
C28H24F3N7O3S
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0451775
15-methylsulfonyl-25-(trifluoromethyl)-2,10,15,17,23,27,28-heptazapentacyclo[22.3.1.13,7.06,10.016,21]nonacosa-1(27),3(29),4,6,16(21),17,19,24(28),25-nonaen-11-one
   Show/Hide
C24H24F3N7O3S
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0516061
N-[3-[[[2-(3-bromoanilino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]-N-prop-2-enylmethanesulfonamide
   Show/Hide
C21H20BrF3N6O2S
 1
1
IC50 = 122 nM
   TI
   LI
   LO
   TS
CP0545412
5-[2-[[[2-(2,3-dihydro-1H-indol-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]-methylamino]methyl]-N-methylsulfonylanilino]pentanoic acid
   Show/Hide
C27H31F3N6O4S
 1
1
IC50 = 201 nM
   TI
   LI
   LO
   TS
CP0545411
5-[2-[[[2-(2,3-dihydro-1H-indol-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]-N-ethylsulfonylanilino]pentanoic acid
   Show/Hide
C27H31F3N6O4S
 1
1
IC50 = 256 nM
   TI
   LI
   LO
   TS
CP0454688
N-[4-[[[2-(3-bromo-4-morpholin-4-ylanilino)-5-(trifluoromethyl)pyrimidin-4-yl]-methylamino]methyl]pyridin-3-yl]-N-prop-2-enylmethanesulfonamide
   Show/Hide
C26H29BrF3N7O3S
 1
1
IC50 = 6625 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
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
   Show/Hide
C21H20F3N7O3S
 3
1 IC50 = 1.4 nM
2 IC50 = 13 nM
3 IC50 = 14 nM
CP0181347
N-[5-(6,7-dimethoxyquinolin-4-yl)oxypyridin-2-yl]-4-(methylamino)-2-oxo-1-phenylpyridine-3-carboxamide
   Show/Hide
C29H25N5O5
 1
1 IC50 = 35 nM
CP0180276
5-benzyl-N-(5-(6,7-dimethoxyquinolin-4-yloxy)pyridin-2-yl)-2-oxo-1-phenyl-1,2-dihydropyridine-3-carboxamide
   Show/Hide
C35H28N4O5
 1
1 IC50 = 49 nM
CP0039510
N-[5-(6,7-dimethoxyquinolin-4-yl)oxypyridin-2-yl]-2-oxo-1-phenyl-5-thiophen-2-ylpyridine-3-carboxamide
   Show/Hide
C32H24N4O5S
 1
1 IC50 = 53 nM
Clinical Information about the Protein
Target 1 ( Focal adhesion kinase 2 (PTK2B) )
Target Type Literature-reported Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06725 Protein-tyrosine kinase 2-beta Mus musculus, Mouse