Target Information

Target General Information

Top

Target ID

T59328 (Former ID: TTDS00355)

Target Name

Epidermal growth factor receptor (EGFR)

Synonyms

Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB

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Gene Name

EGFR

Target Type

Successful target

[1]

Disease

[+] 10 Target-related Diseases

Angina pectoris [ICD-11: BA40]

Breast cancer [ICD-11: 2C60-2C6Y]

Colorectal cancer [ICD-11: 2B91]

Diabetic foot ulcer [ICD-11: BD54]

Ischemia [ICD-11: 8B10-8B11]

Lung cancer [ICD-11: 2C25]

Non-small-cell lung cancer [ICD-11: 2C25]

Renal cell carcinoma [ICD-11: 2C90]

Solid tumour/cancer [ICD-11: 2A00-2F9Z]

Unspecific body region injury [ICD-11: ND56]

Function

Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules. May also activate the NF-kappa-B signaling cascade. Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling. Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin. Plays a role in enhancing learning and memory performance (By similarity).

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BioChemical Class

Kinase

UniProt ID

EGFR_HUMAN

EC Number

EC 2.7.10.1

Sequence

MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

ADReCS ID

BADD_A00924 ; BADD_A01146 ; BADD_A01626 ; BADD_A02005 ; BADD_A05675 ; BADD_A06535

HIT2.0 ID

T43N2D

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 19 Approved Drugs

Amivantamab

Drug Info

Approved

Non-small-cell lung cancer

[2]

BIBW 2992

Drug Info

Approved

Non-small-cell lung cancer

[3], [4]

Cetuximab

Drug Info

Approved

Colorectal cancer

[5], [6]

Dacomitinib

Drug Info

Approved

Non-small-cell lung cancer

[7]

Epidermal growth factor

Drug Info

Approved

Vulnerary

[8]

Erlotinib

Drug Info

Approved

Non-small-cell lung cancer

[6], [9]

Gefitinib

Drug Info

Approved

Solid tumour/cancer

[10], [11]

HEGF

Drug Info

Approved

Diabetic foot ulcer

[12]

Lapatinib

Drug Info

Approved

Breast cancer

[13], [14]

Merimepodib

Drug Info

Approved

Breast cancer

[15]

Necitumumab

Drug Info

Approved

Colorectal cancer

[16], [17]

NERATINIB MALEATE

Drug Info

Approved

HER2/NEU overexpressing breast cancer

[18]

Nitroglycerin

Drug Info

Approved

Diabetic foot ulcer

[12]

Osimertinib

Drug Info

Approved

Non-small-cell lung cancer

[19]

Panitumumab

Drug Info

Approved

Colorectal cancer

[20], [21]

SKI-758

Drug Info

Approved

Ischemia

[8], [22]

Sorafenib

Drug Info

Approved

Renal cell carcinoma

[23], [24]

Vandetanib

Drug Info

Approved

Solid tumour/cancer

[25], [26]

Icotinib hydrochloride

Drug Info

Registered

Non-small-cell lung cancer

[27], [28], [29]

Clinical Trial Drug(s)

[+] 66 Clinical Trial Drugs

A140

Drug Info

Phase 3

Head and neck cancer

[30]

Almonertinib

Drug Info

Phase 3

Non-small-cell lung cancer

[31]

ASP1929

Drug Info

Phase 3

Head and neck cancer

[32]

Bevacizumab + Erlotinib

Drug Info

Phase 3

Metastatic colorectal cancer

[33], [34]

CO-1686

Drug Info

Phase 3

Lung cancer

[35]

DE-766

Drug Info

Phase 3

Non-small-cell lung cancer

[36], [37]

EGF816

Drug Info

Phase 3

Non-small-cell lung cancer

[38]

HKI-272

Drug Info

Phase 3

Breast cancer

[39], [38]

Rindopepimut

Drug Info

Phase 3

Glioblastoma multiforme

[40]

SYM-004

Drug Info

Phase 3

Metastatic colorectal cancer

[38]

Zalutumumab

Drug Info

Phase 3

Head and neck cancer

[41]

Indium-111

Drug Info

Phase 2/3

Solid tumour/cancer

[42]

Varlitinib

Drug Info

Phase 2/3

Metastatic biliary tract neoplasms

[38]

ABT-414

Drug Info

Phase 2

Glioblastoma multiforme

[43], [44]

ASP8273

Drug Info

Phase 2

Non-small-cell lung cancer

[45]

BMS-599626

Drug Info

Phase 2

Solid tumour/cancer

[46], [47]

BMS-690514

Drug Info

Phase 2

Chronic pain

[48]

CetuGEX

Drug Info

Phase 2

Solid tumour/cancer

[49]

CI-1033

Drug Info

Phase 2

Lymphoma

[50], [51]

Depatuxizumab

Drug Info

Phase 2

Glioblastoma of brain

[52]

HER1-VSSP vaccine

Drug Info

Phase 2

Solid tumour/cancer

[53], [54]

HM-78136B

Drug Info

Phase 2

Solid tumour/cancer

[55], [56]

Matuzumab

Drug Info

Phase 2

Gastric adenocarcinoma

[57]

MEHD-7945A

Drug Info

Phase 2

Colorectal cancer

[58], [59]

Pazopanib + Tyverb/Tykerb

Drug Info

Phase 2

Inflammatory breast cancer

[60]

Pelitinib

Drug Info

Phase 2

Lymphoma

[61], [62]

RM-1929

Drug Info

Phase 2

Head and neck cancer

[38], [63]

Tarloxotinib

Drug Info

Phase 2

Non-small-cell lung cancer

[64]

TT-100

Drug Info

Phase 2

Non-small-cell lung cancer

[65]

VATALANIB

Drug Info

Phase 2

Solid tumour/cancer

[66], [67]

AFM24

Drug Info

Phase 1/2

Solid tumour/cancer

[68]

BDTX-189

Drug Info

Phase 1/2

Solid tumour/cancer

[69]

CART-EGFR

Drug Info

Phase 1/2

Solid tumour/cancer

[70]

EGFR CART

Drug Info

Phase 1/2

Colorectal cancer

[71]

EMB-01

Drug Info

Phase 1/2

Neoplasm

[72]

EMD 55900

Drug Info

Phase 1/2

Glioma

[73]

SN-32793

Drug Info

Phase 1/2

Non-small-cell lung cancer

[74]

Sym013

Drug Info

Phase 1/2

Epithelial ovarian cancer

[38]

Sym015

Drug Info

Phase 1/2

Solid tumour/cancer

[63], [38]

TAK-186

Drug Info

Phase 1/2

Aggressive cancer

[75]

ZN-e4

Drug Info

Phase 1/2

Non-small-cell lung cancer

[76]

S-222611

Drug Info

Phase 1b

Malignant solid tumour

[77]

AMG 595

Drug Info

Phase 1

Glioblastoma multiforme

[78]

Anti-EGFR CAR T

Drug Info

Phase 1

Glioma

[79]

Anti-HER3/EGFR DAF

Drug Info

Phase 1

Metastatic epithelial tumour

[80]

AP32788

Drug Info

Phase 1

Non-small-cell lung cancer

[38]

AST-1306

Drug Info

Phase 1

Solid tumour/cancer

[81]

AZD9592

Drug Info

Phase 1

Aggressive cancer

[82]

BCA101

Drug Info

Phase 1

Solid tumour/cancer

[83]

BIBX-1382

Drug Info

Phase 1

Chronic lymphocytic leukaemia

[84], [85]

Cipatinib

Drug Info

Phase 1

Solid tumour/cancer

[86]

CLN-081

Drug Info

Phase 1

Non-small-cell lung cancer

[87]

CUDC-101

Drug Info

Phase 1

Solid tumour/cancer

[88]

CX-904

Drug Info

Phase 1

Colorectal cancer

[89]

D2C7

Drug Info

Phase 1

Glioblastoma of brain

[90]

EGFR806-specific CAR T cell

Drug Info

Phase 1

Atypical teratoid/rhabdoid tumour

[91]

HER-2/HER-1 vaccine

Drug Info

Phase 1

Solid tumour/cancer

[92]

IMGN289

Drug Info

Phase 1

Solid tumour/cancer

[93]

JNJ-26483327

Drug Info

Phase 1

Solid tumour/cancer

[94]

LY3164530

Drug Info

Phase 1

Advanced cancer

[95]

MCLA-158

Drug Info

Phase 1

Solid tumour/cancer

[96]

MM-151

Drug Info

Phase 1

Solid tumour/cancer

[97]

MR1-1

Drug Info

Phase 1

Brain cancer

[98]

PF-05230907

Drug Info

Phase 1

Nontraumatic intracerebral hemorrhage

[99]

SI-B001

Drug Info

Phase 1

Metastatic epithelial tumour

[100]

SYN004

Drug Info

Phase 1

Solid tumour/cancer

[63], [38]

Discontinued Drug(s)

[+] 8 Discontinued Drugs

PKI166

Drug Info

Discontinued in Phase 2

Esophageal cancer

[101], [102]

RG7160

Drug Info

Discontinued in Phase 2

Metastatic colorectal cancer

[103]

AZD4769

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[104]

PD-153035

Drug Info

Discontinued in Phase 1

Psoriasis vulgaris

[105]

TAK165

Drug Info

Discontinued in Phase 1

Solid tumour/cancer

[106], [107]

AZD-9935

Drug Info

Terminated

Solid tumour/cancer

[111]

CGP-52411

Drug Info

Terminated

Solid tumour/cancer

[112]

Heparin-EGF-like factor

Drug Info

Terminated

Gastrointestinal disease

[113], [114]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

111In-hEGF

Drug Info

Preclinical

Breast cancer

[108], [109]

EGFR/IGFR tandem adnectin

Drug Info

Preclinical

Solid tumour/cancer

[110]

Mode of Action

[+] 6 Modes of Action

Inhibitor

[+] 128 Inhibitor drugs

Amivantamab

Drug Info

[115]

BIBW 2992

Drug Info

[116]

Erlotinib

Drug Info

[120]

Gefitinib

Drug Info

[121], [122]

Lapatinib

Drug Info

[123], [124]

Merimepodib

Drug Info

[125]

Osimertinib

Drug Info

[127]

SKI-758

Drug Info

[129]

Sorafenib

Drug Info

[130]

Vandetanib

Drug Info

[131], [132]

Almonertinib

Drug Info

[134]

ASP1929

Drug Info

[135]

Bevacizumab + Erlotinib

Drug Info

[136]

EGF816

Drug Info

[138]

HKI-272

Drug Info

[139]

ASP8273

Drug Info

[145]

BMS-599626

Drug Info

[146], [131]

BMS-690514

Drug Info

[147]

CI-1033

Drug Info

[131]

HM-78136B

Drug Info

[38], [148]

Pazopanib + Tyverb/Tykerb

Drug Info

[125]

Tarloxotinib

Drug Info

[152]

TT-100

Drug Info

[153]

VATALANIB

Drug Info

[139]

BDTX-189

Drug Info

[155]

EMB-01

Drug Info

[156]

SN-32793

Drug Info

[119]

TAK-186

Drug Info

[157]

ZN-e4

Drug Info

[158]

S-222611

Drug Info

[77]

AP32788

Drug Info

[38]

BCA101

Drug Info

[83]

CLN-081

Drug Info

[166]

IMGN289

Drug Info

[169]

JNJ-26483327

Drug Info

[170]

MCLA-158

Drug Info

[171]

PF-05230907

Drug Info

[173]

SYN004

Drug Info

[63]

Pyrrolo[2,3-d]pyrimidine derivative 24

Drug Info

[175]

AZD4769

Drug Info

[132]

TAK165

Drug Info

[131]

EGFR/IGFR tandem adnectin

Drug Info

[180]

CGP-52411

Drug Info

[182]

CGP-53353

Drug Info

[183]

(3-Bromo-phenyl)-(5-nitro-quinazolin-4-yl)-amine

Drug Info

[184]

(3-Bromo-phenyl)-quinazolin-4-yl-amine

Drug Info

[185]

(E)-5-(4-Hydroxybenzylidene)-1-phenethylhydantoin

Drug Info

[186]

(S)-benzyl 4-chloro-3-oxobutan-2-ylcarbamate

Drug Info

[187]

10-hydroxy-18-methoxybetaenone

Drug Info

[188]

2-(4,5-Dihydroxy-indan-1-ylidene)-malononitrile

Drug Info

[189]

2-(5,6-Dihydroxy-indan-1-ylidene)-malononitrile

Drug Info

[189]

2-benzoyl-3-(3,4-dihydroxyphenyl)acrylonitrile

Drug Info

[187]

2-cyano-3-(3,4-dihydroxyphenyl)acrylamide

Drug Info

[187]

2-methoxy-4-(2-nitrovinyl)phenol

Drug Info

[187]

3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione

Drug Info

[190]

3,4-diphenyl-1H-pyrrole-2,5-dione

Drug Info

[190]

3-(3-Chloro-phenyl)-5,7-dihydroxy-chromen-4-one

Drug Info

[191]

3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione

Drug Info

[190]

3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione

Drug Info

[190]

3-Pyridin-4-yl-quinoline-6,7-diol

Drug Info

[192]

4-(2-nitroprop-1-enyl)benzene-1,2-diol

Drug Info

[187]

4-(2-nitrovinyl)benzene-1,2-diol

Drug Info

[187]

4-(2-nitrovinyl)phenol

Drug Info

[187]

4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline

Drug Info

[193]

4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline

Drug Info

[193]

4-(3-Bromo-phenylamino)-quinazoline-6,7-diol

Drug Info

[185]

4-(4-(2-nitrovinyl)phenoxysulfonyl)benzoic acid

Drug Info

[187]

4-(5-Bromoindole-3-yl)-6,7-dimethoxyquinazoline

Drug Info

[194]

4-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide

Drug Info

[195]

4-biphenyl-2-ylethynyl-6,7-dimethoxy-quinazoline

Drug Info

[196]

4557W

Drug Info

[197]

5,6-Bis-p-tolylamino-isoindole-1,3-dione

Drug Info

[183]

5-acrylamido-N-(3-bromophenyl)-2-hydroxybenzamide

Drug Info

[195]

6,7-diethoxy-4-(4-phenylbut-1-enyl)quinazoline

Drug Info

[196]

6,7-diethoxy-4-(5-phenylpent-1-enyl)quinazoline

Drug Info

[196]

6,7-diethoxy-4-styrylquinazoline

Drug Info

[196]

6,7-dimethoxy-4-(2-phenylethynyl)quinazoline

Drug Info

[196]

6,7-dimethoxy-4-(3-phenoxyprop-1-ynyl)quinazoline

Drug Info

[196]

6,7-dimethoxy-4-(4-phenylbut-1-ynyl)quinazoline

Drug Info

[196]

6,7-dimethoxy-N-m-tolylquinazolin-4-amine

Drug Info

[198]

6-chloro-N-(3-chlorophenyl)quinazolin-4-amine

Drug Info

[199]

AG 112

Drug Info

[200]

AG 9

Drug Info

[200]

AG-213

Drug Info

[194]

AG-538

Drug Info

[187]

Benzo[g]quinazolin-4-yl-(3-bromo-phenyl)-amine

Drug Info

[185]

Benzyl-quinazolin-4-yl-amine

Drug Info

[184]

BPIQ-I

Drug Info

[185]

CL-387785

Drug Info

[198]

Cochliobolic acid

Drug Info

[201]

EGFR inhibitor

Drug Info

[202]

Epitinib

Drug Info

[119]

HDS-029

Drug Info

[203]

HKI-9924129

Drug Info

[204]

HM-61713B

Drug Info

[119]

HTS-00213

Drug Info

[198]

HTS-02876

Drug Info

[198]

HTS-05058

Drug Info

[202]

LAVENDUSTIN A

Drug Info

[205]

100

MDP-01

Drug Info

[119]

101

MT-062

Drug Info

[119]

102

N*4*-(3-Bromo-phenyl)-quinazoline-4,6,7-triamine

Drug Info

[185]

103

N*4*-(3-Bromo-phenyl)-quinazoline-4,6-diamine

Drug Info

[207]

104

N*4*-(3-Bromo-phenyl)-quinazoline-4,7-diamine

Drug Info

[184]

105

N*4*-Benzyl-pyrido[4,3-d]pyrimidine-4,7-diamine

Drug Info

[208]

106

N-(4-(phenylamino)quinazolin-6-yl)acrylamide

Drug Info

[209]

107

N-(4-m-Tolylamino-quinazolin-6-yl)-acrylamide

Drug Info

[210]

108

N-(4-m-Tolylamino-quinazolin-7-yl)-acrylamide

Drug Info

[210]

109

N4-(3-chlorophenyl)quinazoline-4,6-diamine

Drug Info

[211]

110

N4-(3-methylphenyl)-4,6-quinazolinediamine

Drug Info

[212]

111

NRC-2694

Drug Info

[119]

112

ON-128

Drug Info

[119]

113

OSI-75

Drug Info

[213]

114

PD-0166326

Drug Info

[204]

115

PD-0173956

Drug Info

[204]

116

PD-158780

Drug Info

[208]

117

PD-168393

Drug Info

[209]

118

PD182905

Drug Info

[214]

119

PMID24915291C38

Drug Info

[216]

120

PMID8568816C56

Drug Info

[217]

121

PP121

Drug Info

[218]

122

RG-50810

Drug Info

[187]

123

RM-6427

Drug Info

[119]

124

Ro-4396686

Drug Info

[219]

125

Theliatinib

Drug Info

[119]

126

Tyrphostin ag-1478

Drug Info

[191]

127

WHI-P154

Drug Info

[220]

128

WZ-3146

Drug Info

[119]

Antagonist

[+] 13 Antagonist drugs

Dacomitinib

Drug Info

[119]

NERATINIB MALEATE

Drug Info

[18]

Icotinib hydrochloride

Drug Info

[133]

Depatuxizumab

Drug Info

[63]

RM-1929

Drug Info

[38]

Sym013

Drug Info

[63], [38]

Sym015

Drug Info

[63]

BIBX-1382

Drug Info

[165]

MM-151

Drug Info

[63]

AZD-9935

Drug Info

[181]

EDP-13

Drug Info

[119]

IPS-01003

Drug Info

[119]

RX-1792

Drug Info

[119]

Modulator

[+] 27 Modulator drugs

Epidermal growth factor

Drug Info

[119]

Necitumumab

Drug Info

[126]

CO-1686

Drug Info

[137]

DE-766

Drug Info

[119]

Rindopepimut

Drug Info

[126]

Varlitinib

Drug Info

[142]

MEHD-7945A

Drug Info

[142], [150]

Pelitinib

Drug Info

[151]

AMG 595

Drug Info

[159]

Anti-HER3/EGFR DAF

Drug Info

[160]

AST-1306

Drug Info

[161], [162], [163]

Cipatinib

Drug Info

[142]

CUDC-101

Drug Info

[88]

LY3164530

Drug Info

[150]

MR1-1

Drug Info

[172]

PKI166

Drug Info

[176]

RG7160

Drug Info

[177]

PD-153035

Drug Info

[178]

111In-hEGF

Drug Info

[179]

Heparin-EGF-like factor

Drug Info

[113], [114]

AGT-2000

Drug Info

[119]

AL-6802

Drug Info

[119]

LA22-radioimmunoconjugates

Drug Info

[119]

MG-111

Drug Info

[206]

PF 5208766

Drug Info

[215]

SYM-011

Drug Info

[119]

TGF alpha

Drug Info

[119]

Activator

[+] 2 Activator drugs

HEGF

Drug Info

[12]

Nitroglycerin

Drug Info

[12]

Suppressor

[+] 1 Suppressor drugs

Panitumumab

Drug Info

[128]

CAR-T-Cell-Therapy

[+] 4 CAR-T-Cell-Therapy drugs

CART-EGFR

Drug Info

[70]

EGFR CART

Drug Info

[71]

Anti-EGFR CAR T

Drug Info

[79]

EGFR806-specific CAR T cell

Drug Info

[91]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

Top

Ligand Name: Lapatinib

Ligand Info

Structure Description

EGFR kinase domain complexed with a quinazoline inhibitor- GW572016

PDB:1XKK

Method

X-ray diffraction

Resolution

2.40 Å

Mutation

[222]

PDB Sequence

ALLRILKETE

⁷¹¹

FKKIKVLGSG

⁷²¹

AFGTVYKGLW

⁷³¹

IPVKIPVAIK

⁷⁴⁵

ELREKANKEI

⁷⁵⁹

LDEAYVMASV

⁷⁶⁹

DNPHVCRLLG

⁷⁷⁹

ICLTSTVQLI

⁷⁸⁹

TQLMPFGCLL

⁷⁹⁹

DYVREHKDNI

⁸⁰⁹

GSQYLLNWCV

⁸¹⁹

QIAKGMNYLE

⁸²⁹

DRRLVHRDLA

⁸³⁹

ARNVLVKTPQ

⁸⁴⁹

HVKITDFGLA

⁸⁵⁹

KLLGAEEKVP

⁸⁷⁷

IKWMALESIL

⁸⁸⁷

HRIYTHQSDV

⁸⁹⁷

WSYGVTVWEL

⁹⁰⁷

MTFGSKPYDG

⁹¹⁷

IPASEISSIL

⁹²⁷

EKGERLPQPP

⁹³⁷

ICTIDVYMIM

⁹⁴⁷

VKCWMIDADS

⁹⁵⁷

RPKFRELIIE

⁹⁶⁷

FSKMARDPQR

⁹⁷⁷

YLVIQGDERM

⁹⁸⁷

SNFYRALMDE

¹⁰⁰⁴

VVDADEYLI

Residue

Distance (Å)

LEU718

3.870

GLY719

4.124

VAL726

3.854

ALA743

3.334

ILE744

4.349

LYS745

3.414

MET766

3.317

CYS775

3.424

ARG776

3.123

LEU777

3.371

LEU788

3.100

ILE789

4.160

THR790

3.138

GLN791

3.195

Residue

Distance (Å)

LEU792

3.715

MET793

2.960

GLY796

3.809

CYS797

3.130

LEU799

3.534

ASP800

3.057

ARG803

3.623

ARG841

4.149

LEU844

3.375

THR854

3.596

ASP855

3.483

PHE856

3.479

LEU858

3.841

MET1002

4.023

Ligand Name: Brigatinib

Ligand Info

Structure Description

Studies Towards a Reversible EGFR C797S Triple Mutant Inhibitor Series

PDB:7AEM

Method

X-ray diffraction

Resolution

2.65 Å

Mutation

[223]

PDB Sequence

SGEAPNQALL

⁷⁰⁴

RILKETEFKK

⁷¹⁴

IKVLGSGAFG

⁷²⁴

TVYKGLWIPE

⁷³⁴

GEKVKIPVAI

⁷⁴⁴

KELATSPKAN

⁷⁵⁶

KEILDEAYVM

⁷⁶⁶

ASVDNPHVCR

⁷⁷⁶

LLGICLTSTV

⁷⁸⁶

QLITQLMPFG

⁷⁹⁶

CLLDYVREHK

⁸⁰⁶

DNIGSQYLLN

⁸¹⁶

WCVQIAKGMN

⁸²⁶

YLEDRRLVHR

⁸³⁶

DLAARNVLVK

⁸⁴⁶

TPQHVKITDF

⁸⁵⁶

GLAKLLGAEE

⁸⁶⁶

KEYHAEGGKV

⁸⁷⁶

PIKWMALESI

⁸⁸⁶

LHRIYTHQSD

⁸⁹⁶

VWSYGVTVWE

⁹⁰⁶

LMTFGSKPYD

⁹¹⁶

GIPASEISSI

⁹²⁶

LEKGERLPQP

⁹³⁶

PICTIDVYMI

⁹⁴⁶

MVKCWMIDAD

⁹⁵⁶

SRPKFRELII

⁹⁶⁶

EFSKMARDPQ

⁹⁷⁶

RYLVIQGDER

⁹⁸⁶

MHLPLMDEED

¹⁰⁰⁶

MDDVVDADEY

¹⁰¹⁶

Residue

Distance (Å)

LEU718

3.663

GLY719

3.649

PHE723

3.562

VAL726

3.766

ALA743

3.266

LYS745

4.226

THR790

3.893

GLN791

3.498

LEU792

3.620

MET793

2.921

PRO794

3.438

Residue

Distance (Å)

PHE795

4.917

GLY796

3.086

CYS797

4.105

ASP800

4.640

GLU804

3.632

ARG841

3.627

ASN842

4.415

LEU844

3.425

THR854

4.115

ASP855

4.115

Click to View More Binding Site Information of This Target with Different Ligands

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues. The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Tissue Distribution Human Pathway Affiliation Biological Network Descriptors

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.

The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Tissue Distribution

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Mixed lineage kinase 1 (MAP3K9)	PF00069 ; PF14604	32.432 (96/296)	4.02E-32
Serine/threonine-protein kinase 25 (STK25)	PF00069	32.843 (67/204)	1.05E-20
Serine/threonine-protein kinase PAK 3 (PAK3)	PF00786 ; PF00069	29.630 (80/270)	1.09E-18
MST-1 protein kinase (STK4)	PF11629 ; PF00069	29.858 (63/211)	5.30E-18
Ribosomal protein S6 kinase alpha-1 (RSK1)	PF00069 ; PF00433	28.879 (67/232)	9.35E-18
PAK-1 protein kinase (PAK1)	PF00786 ; PF00069	27.778 (75/270)	1.38E-17
Serine/threonine-protein kinase 24 (STK24)	PF00069	30.500 (61/200)	2.86E-17
Serine/threonine-protein kinase 26 (STK26)	PF00069	31.343 (63/201)	4.26E-17
Serine/threonine-protein kinase 3 (STK3)	PF11629 ; PF00069	28.910 (61/211)	8.72E-17
Ste-20-related kinase (STK39)	PF12202 ; PF00069	28.509 (65/228)	1.02E-16
PKC-delta-interacting protein kinase (RIPK4)	PF12796 ; PF00069	29.286 (82/280)	1.49E-16
Ribosomal protein S6 kinase alpha-3 (RSK3)	PF00069 ; PF00433	27.826 (64/230)	1.54E-16
Ribosomal protein S6 kinase alpha-2 (RSK2)	PF00069 ; PF00433	28.139 (65/231)	1.87E-16
ERK activator kinase 5 (MAP2K5)	PF00564 ; PF00069	28.505 (61/214)	2.01E-16
NIMA-related kinase 6 (NEK6)	PF00069	25.641 (60/234)	3.21E-16
Unc-51 like kinase 3 (ULK3)	PF04212 ; PF00069	26.275 (67/255)	3.48E-16
PAK-2 protein kinase (PAK2)	PF00786 ; PF00069	27.407 (74/270)	4.85E-16
SPS1/STE20-related protein kinase YSK4 (YSK4)	PF00069	29.268 (60/205)	5.44E-16
NIMA-related kinase 7 (NEK7)	PF00069	24.464 (57/233)	7.09E-16
MAPK/ERK kinase kinase 1 (MAP3K1)	PF00069	23.985 (65/271)	1.03E-15
Microtubule affinity regulating kinase 3 (MARK3)	PF02149 ; PF00069 ; PF00627 More >>	26.840 (62/231)	1.04E-15
Ribosomal protein S6 kinase alpha-6 (RSK6)	PF00069 ; PF00433	28.085 (66/235)	1.07E-15
Serine/threonine-protein kinase ULK1 (ULK1)	PF12063 ; PF00069	24.898 (61/245)	2.21E-15
Hormonally up-regulated neu tumor-associated kinase (HUNK)	PF00069	29.048 (61/210)	2.23E-15
Serine/threonine-protein kinase Nek11 (NEK11)	PF00069	28.643 (57/199)	2.56E-15
Oxidative stress responsive 1 (OXSR1)	PF12202 ; PF00069	27.193 (62/228)	3.42E-15
WNK lysine-deficient protein kinase 3 (WNK3)	PF12202 ; PF00069	30.846 (62/201)	4.16E-15
Apoptosis signal-regulating kinase 2 (MAP3K6)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	26.333 (79/300)	8.89E-15
Serine/threonine-protein kinase ULK2 (ULK2)	PF12063 ; PF00069	23.750 (57/240)	1.10E-14
ERK activator kinase 1 (MEK1)	PF00069	27.386 (66/241)	1.66E-14
Aurora kinase A (AURKA)	PF00069	23.574 (62/263)	1.83E-14
Apoptosis signal-regulating kinase 1 (MAP3K5)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	27.473 (75/273)	1.96E-14
ERK activator kinase 7 (MAP2K7)	PF00069	25.856 (68/263)	2.51E-14
Serine/threonine-protein kinase WNK1 (WNK1)	PF12202 ; PF00069	30.622 (64/209)	2.66E-14
Salt-inducible kinase 2 (SIK2)	PF00069	29.435 (73/248)	3.32E-14
MAP/microtubule affinity-regulating kinase 4 (MARK4)	PF02149 ; PF00069 ; PF00627 More >>	25.877 (59/228)	3.59E-14
Serine/threonine-protein kinase 10 (STK10)	PF00069 ; PF12474	28.426 (56/197)	3.70E-14
Protein kinase C alpha (PRKCA)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	26.172 (67/256)	4.16E-14
Serine/threonine-protein kinase 33 (STK33)	PF00069	29.870 (69/231)	4.28E-14
Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4)	PF00069	28.837 (62/215)	4.46E-14
MAPK/ERK kinase kinase 3 (MAP3K3)	PF00564 ; PF00069	27.206 (74/272)	4.98E-14
Dual specificity mitogen-activated protein kinase kinase 6 (MAP2K6)	PF00069	27.206 (74/272)	5.20E-14
Serine/threonine-protein kinase WNK2 (WNK2)	PF12202 ; PF00069	30.288 (63/208)	5.99E-14
Cyclin-dependent kinase 6 (CDK6)	PF00069	26.457 (59/223)	7.82E-14
ERK activator kinase 2 (MEK2)	PF00069	26.877 (68/253)	7.95E-14
Serine/threonine-protein kinase Nek5 (NEK5)	PF00069	22.745 (58/255)	9.01E-14
Receptor-interacting serine/threonine-protein kinase 3 (RIPK3)	PF00069 ; PF12721	27.241 (79/290)	9.07E-14
Phosphoinositide dependent protein kinase-1 (PDPK1)	PF14593 ; PF00069	27.962 (59/211)	9.93E-14
SNF-related serine/threonine-protein kinase (SNRK)	PF00069	27.907 (60/215)	1.23E-13
Serine/threonine-protein kinase Nek8 (NEK8)	PF00069 ; PF00415	26.923 (56/208)	1.27E-13
MAPK/ERK kinase kinase 2 (MAP3K2)	PF00564 ; PF00069	27.338 (76/278)	1.64E-13
Testis-specific serine/threonine-protein kinase 4 (TSSK4)	PF00069	27.950 (45/161)	2.76E-13
Cyclin-dependent kinase 3 (CDK3)	PF00069	26.667 (56/210)	3.36E-13
Myosin-IIIa (MYO3A)	PF00612 ; PF00063 ; PF00069 More >>	26.966 (72/267)	3.77E-13
Cyclin-dependent kinase 2 (CDK2)	PF00069	26.214 (54/206)	3.79E-13
Serine/threonine-protein kinase MARK2 (MARK2)	PF02149 ; PF00069 ; PF00627 More >>	26.106 (59/226)	5.02E-13
Putative 3-phosphoinositide-dependent protein kinase 2 (PDPK2P)	PF00069	27.488 (58/211)	5.12E-13
Protein kinase C theta (PRKCQ)	PF00130 ; PF00069 ; PF00433 More >>	24.055 (70/291)	5.29E-13
STE20-related serine/threonine-protein kinase (SLK)	PF00069 ; PF12474	26.482 (67/253)	5.96E-13
Serine/threonine-protein kinase 32A (STK32A)	PF00069	25.359 (53/209)	6.39E-13
NUAK family SNF1-like kinase 2 (NUAK2)	PF00069	26.295 (66/251)	6.69E-13
Mitogen-activated protein kinase kinase kinase 15 (MAP3K15)	PF19039 ; PF20309 ; PF20302 ; PF13281 ; PF00069 More >>	29.703 (60/202)	7.97E-13
Serine/threonine-protein kinase D2 (PRKD2)	PF00130 ; PF00069	29.327 (61/208)	8.17E-13
Serine/threonine-protein kinase MARK1 (MARK1)	PF02149 ; PF00069 ; PF00627 More >>	25.664 (58/226)	9.32E-13
Ribosomal protein S6 kinase beta-2 (RPS6KB2)	PF00069 ; PF00433	25.207 (61/242)	1.09E-12
Fused homolog (STK36)	PF13646 ; PF00069	23.744 (52/219)	1.60E-12
Polo-like kinase 4 (PLK4)	PF00069 ; PF18190 ; PF18409 More >>	27.273 (57/209)	2.17E-12
Cyclin-dependent kinase 1 (CDK1)	PF00069	26.442 (55/208)	2.25E-12
Leucine-rich repeat serine/threonine-protein kinase 1 (LRRK1)	PF12796 ; PF16095 ; PF00069 ; PF08477 More >>	25.260 (73/289)	2.36E-12
Serine/threonine-protein kinase WNK4 (WNK4)	PF12202 ; PF00069	27.805 (57/205)	2.65E-12
Serine/threonine-protein kinase Nek3 (NEK3)	PF00069	24.757 (51/206)	2.95E-12
Leucine-rich repeat kinase 2 (LRRK2)	PF16095 ; PF12799 ; PF13855 ; PF00069 ; PF08477 More >>	27.311 (65/238)	3.29E-12
Cyclin-dependent kinase 7 (CDK7)	PF00069	25.000 (52/208)	3.39E-12
Protein kinase D (PRKD1)	PF00130 ; PF00169 ; PF00069 More >>	28.365 (59/208)	3.42E-12
cAMP-dependent protein kinase catalytic subunit PRKX (PRKX)	PF00069	23.451 (53/226)	5.05E-12
Serine/threonine-protein kinase Nek4 (NEK4)	PF00069	24.046 (63/262)	7.37E-12
cAMP-dependent protein kinase catalytic subunit gamma (PRKACG)	PF00069	22.530 (57/253)	8.74E-12
Cyclin-dependent kinase 5 (CDK5)	PF00069	23.707 (55/232)	9.04E-12
Putative serine/threonine-protein kinase PRKY (PRKY)	PF00069	23.744 (52/219)	9.18E-12
Maternal embryonic leucine zipper kinase (MELK)	PF02149 ; PF00069	25.296 (64/253)	9.60E-12
SIK family kinase 3 (SIK3)	PF00069	25.442 (72/283)	9.78E-12
Tyrosine-protein kinase EIF2AK2 (p68)	PF00035 ; PF00069	24.621 (65/264)	1.16E-11
Serine/threonine-protein kinase Nek9 (NEK9)	PF00069 ; PF00415	23.864 (63/264)	1.26E-11
Ribosomal protein S6 kinase beta-1 (S6K1)	PF00069 ; PF00433	25.397 (64/252)	1.28E-11
Protein kinase C delta (PRKCD)	PF00130 ; PF00069 ; PF00433 More >>	28.302 (60/212)	1.49E-11
Serine/threonine-protein kinase Nek10 (NEK10)	PF00069	25.926 (70/270)	1.54E-11
5'-AMP-activated protein kinase catalytic subunit alpha-1 (PRKAA1)	PF16579 ; PF00069	29.064 (59/203)	1.56E-11
Omphalocele kinase 1 (NUAK1)	PF00069	23.843 (67/281)	1.62E-11
Protein kinase C beta (PRKCB)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	24.473 (58/237)	1.64E-11
Cyclin-dependent kinase 20 (CDK20)	PF00069	25.616 (52/203)	1.74E-11
Myosin light chain kinase 3 (MYLK3)	PF00069	25.097 (65/259)	1.93E-11
Protein kinase G1 (PRKG1)	PF00027 ; PF16808 ; PF00069 More >>	23.810 (55/231)	2.01E-11
cAMP-dependent protein kinase catalytic subunit alpha (PRKACA)	PF00069	23.810 (55/231)	2.09E-11
Serine/threonine-protein kinase D3 (PRKD3)	PF00130 ; PF00169 ; PF00069 More >>	27.536 (57/207)	2.14E-11
Yet another novel kinase 2 (STK32B)	PF00069	22.530 (57/253)	2.17E-11
Cyclin-dependent kinase 15 (CDK15)	PF00069	23.894 (54/226)	2.59E-11
Aurora kinase C (AURKC)	PF00069	25.000 (61/244)	3.31E-11
Cyclin-dependent kinase 4 (CDK4)	PF00069	25.778 (58/225)	3.89E-11
TRAF2 and NCK interacting kinase (TNIK)	PF00780 ; PF00069	24.885 (54/217)	4.67E-11
Serine/threonine-protein kinase pim-2 (PIM2)	PF00069	25.279 (68/269)	4.68E-11
Cyclin-dependent kinase 14 (CDK14)	PF00069	25.490 (52/204)	8.38E-11
5'-AMP-activated protein kinase catalytic subunit alpha-2 (PRKAA2)	PF16579 ; PF00069	24.415 (73/299)	8.46E-11
Cyclin-dependent kinase 17 (CDK17)	PF12330 ; PF00069	25.490 (52/204)	8.52E-11
Cyclin-dependent kinase-like 2 (CDKL2)	PF00069	23.077 (81/351)	1.01E-10
cAMP-dependent protein kinase catalytic subunit beta (PRKACB)	PF00069	24.286 (51/210)	1.27E-10
Myosin light chain kinase family member 4 (MYLK4)	PF00069	25.197 (64/254)	1.39E-10
Misshapen-like kinase 1 (MINK1)	PF00780 ; PF00069	25.926 (56/216)	1.49E-10
Putative serine/threonine-protein kinase SIK1B (SIK1B)	PF00069	26.432 (60/227)	1.58E-10
Salt-inducible kinase 1 (SIK1)	PF00069	26.432 (60/227)	1.66E-10
Protein kinase G2 (PRKG2)	PF00027 ; PF00069	23.443 (64/273)	1.66E-10
Ribosomal protein S6 kinase alpha-5 (RSK5)	PF00069 ; PF00433	29.004 (67/231)	1.66E-10
Testis-specific serine/threonine-protein kinase 6 (TSSK6)	PF00069	26.293 (61/232)	2.41E-10
Cyclin-dependent kinase-like 3 (CDKL3)	PF00069	26.047 (56/215)	2.46E-10
Extracellular signal-regulated kinase 1 (ERK1)	PF00069	23.153 (47/203)	2.52E-10
NIMA-related kinase 1 (NEK1)	PF00069	23.415 (48/205)	3.83E-10
Proto-oncogene serine/threonine-protein kinase mos (MOS)	PF00069	22.867 (67/293)	3.86E-10
Death-associated protein kinase 3 (DAPK3)	PF00069	28.169 (60/213)	3.94E-10
Serine/threonine-protein kinase TAO2 (TAOK2)	PF00069	26.961 (55/204)	4.37E-10
Death-associated protein kinase 2 (DAPK2)	PF00069	27.155 (63/232)	4.72E-10
Protein kinase C iota (PRKCI)	PF00130 ; PF00564 ; PF00069 ; PF00433 More >>	23.207 (55/237)	4.91E-10
TAO kinase 1 (TAOK1)	PF00069	26.866 (54/201)	5.33E-10
BR serine/threonine kinase 1 (BRSK1)	PF00069	25.893 (58/224)	5.93E-10
Serine/threonine-protein kinase Sgk3 (SGK3)	PF00069 ; PF00433 ; PF00787 More >>	26.190 (55/210)	6.03E-10
Myosin-IIIb (MYO3B)	PF00612 ; PF00063 ; PF00069 More >>	25.000 (69/276)	6.26E-10
Serine/threonine-protein kinase Chk2 (RAD53)	PF00498 ; PF00069	24.172 (73/302)	7.81E-10
Microtubule-associated serine/threonine-protein kinase 3 (MAST3)	PF08926 ; PF17820 ; PF02163 ; PF00069 More >>	23.643 (61/258)	7.88E-10
Cyclin-dependent kinase 16 (CDK16)	PF12330 ; PF00069	26.087 (54/207)	9.53E-10
Mitogen-activated protein kinase 15 (MAPK15)	PF00069	27.143 (57/210)	1.00E-09
Serine/threonine-protein kinase Sgk1 (SGK1)	PF00069 ; PF00433	24.675 (57/231)	1.07E-09
Serine/threonine-protein kinase ICK (CILK1)	PF00069	26.577 (59/222)	1.26E-09
BR serine/threonine kinase 2 (BRSK2)	PF00069	26.364 (58/220)	1.30E-09
Myosin light kinase (MYLK)	PF16620 ; PF00041 ; PF07679 ; PF00069 More >>	25.243 (52/206)	1.37E-09
Protein kinase C gamma (PRKCG)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	29.268 (36/123)	1.49E-09
Protein kinase C zeta (PRKCZ)	PF00130 ; PF00564 ; PF00069 ; PF00433 More >>	23.950 (57/238)	1.54E-09
Mitogen-activated protein kinase 13 (MAPK13)	PF00069	28.287 (71/251)	1.57E-09
MAP kinase p38 (MAPK12)	PF00069	30.097 (62/206)	1.62E-09
Dual specificity mitogen-activated protein kinase kinase 3 (MAP2K3)	PF00069	28.511 (67/235)	1.66E-09
Ribosomal protein S6 kinase alpha-4 (RPS6KA4)	PF00069 ; PF00433	27.907 (60/215)	1.88E-09
MEK kinase kinase 4 (MAP4K4)	PF00780 ; PF00069	25.000 (54/216)	1.94E-09
Protein kinase N1 (PKN1)	PF02185 ; PF00069 ; PF00433 More >>	26.667 (72/270)	1.96E-09
Microtubule-associated serine/threonine-protein kinase 4 (MAST4)	PF08926 ; PF17820 ; PF02163 ; PF00069 More >>	23.077 (63/273)	2.20E-09
Serine/threonine-protein kinase H2 (PSKH2)	PF00069	25.108 (58/231)	2.48E-09
Serine/threonine-protein kinase PAK 5 (PAK5)	PF00786 ; PF00069	23.429 (41/175)	2.64E-09
Nik-related protein kinase (NRK)	PF00780 ; PF00069	30.827 (41/133)	2.89E-09
Serine/threonine-protein kinase PLK3 (PLK3)	PF00069 ; PF00659	24.878 (51/205)	3.35E-09
Calcium/calmodulin-dependent protein kinase type 1G (CAMK1G)	PF00069	26.733 (54/202)	3.52E-09
Protein kinase C eta type (PRKCH)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	22.981 (74/322)	3.71E-09
Cyclin-dependent kinase 18 (CDK18)	PF00069	24.390 (50/205)	4.09E-09
Death-associated protein kinase 1 (DAPK1)	PF00023 ; PF12796 ; PF13637 ; PF00531 ; PF00069 More >>	27.751 (58/209)	5.48E-09
Myosin light chain kinase 2 (MYLK2)	PF00069	26.829 (55/205)	5.55E-09
Serine/threonine-protein kinase PAK 6 (PAK6)	PF00786 ; PF00069	24.500 (49/200)	6.08E-09
Serine/threonine-protein kinase 32C (STK32C)	PF00069	21.333 (48/225)	7.43E-09
Cytoplasmic DRAK1 (STK17A)	PF00069	27.053 (56/207)	9.17E-09
Microtubule-associated serine/threonine-protein kinase 1 (MAST1)	PF08926 ; PF17820 ; PF00069 More >>	24.895 (59/237)	9.27E-09
Cyclin-dependent kinase 13 (CDK13)	PF12330 ; PF00069	24.766 (53/214)	1.17E-08
MAPK/ERK kinase kinase 4 (MAP3K4)	PF19431 ; PF00069	24.878 (51/205)	1.24E-08
Calcium/calmodulin-dependent protein kinase type 1 (CAMK1)	PF00069	26.786 (60/224)	1.26E-08
Extracellular signal-regulated kinase 2 (ERK2)	PF00069	21.675 (44/203)	1.36E-08
Microtubule-associated serine/threonine-protein kinase 2 (MAST2)	PF08926 ; PF17820 ; PF00069 More >>	24.242 (56/231)	1.53E-08
MEK kinase kinase 3 (MAP4K3)	PF00780 ; PF00069	25.446 (57/224)	1.65E-08
Cyclin-dependent kinase 12 (CDK12)	PF00069	24.889 (56/225)	1.84E-08
Inhibitor of nuclear factor kappa-B kinase beta (IKKB)	PF18397 ; PF12179 ; PF00069 More >>	25.439 (58/228)	1.92E-08
Stress-activated protein kinase 2a (p38 alpha)	PF00069	28.302 (60/212)	1.94E-08
Extracellular signal-regulated kinase 5 (ERK5)	PF00069	24.057 (51/212)	2.25E-08
PRKR-like endoplasmic reticulum kinase (PERK)	PF00069	31.731 (33/104)	2.31E-08
NIMA-related kinase 2 (NEK2)	PF00069	22.097 (59/267)	2.74E-08
Testis-specific serine kinase 2 (TSSK2)	PF00069	25.847 (61/236)	2.74E-08
Cyclin-dependent kinase 9 (CDK9)	PF00069	22.749 (48/211)	3.56E-08
Glycogen synthase kinase-3 beta (GSK-3B)	PF00069	25.664 (58/226)	4.72E-08
Serine/threonine-protein kinase greatwall (MASTL)	PF00069	27.389 (43/157)	6.06E-08
Glycogen synthase kinase-3 alpha (GSK-3A)	PF00069	25.446 (57/224)	6.85E-08
PDZ binding kinase (PBK)	PF00069	25.150 (42/167)	6.89E-08
TAO kinase 3 (TAOK3)	PF00069	27.692 (54/195)	8.14E-08
MEK kinase kinase 1 (MAP4K1)	PF00780 ; PF00069	23.913 (55/230)	8.27E-08
Calcium/calmodulin-dependent protein kinase type IV (CAMK4)	PF00069	28.218 (57/202)	8.94E-08
PAK-4 protein kinase (PAK4)	PF00786 ; PF00069	23.429 (41/175)	9.16E-08
Serine/threonine-protein kinase MAK (MAK)	PF00069	24.623 (49/199)	9.37E-08
Serine/threonine-protein kinase NLK (NLK)	PF00069	25.248 (51/202)	1.01E-07
NDR1 protein kinase (STK38)	PF00069 ; PF00433	22.330 (69/309)	1.05E-07
Stress-activated protein kinase JNK3 (JNK3)	PF00069	27.885 (58/208)	1.26E-07
Serine/threonine-protein kinase Sgk2 (SGK2)	PF00069 ; PF00433	22.807 (52/228)	1.40E-07
Stress-activated protein kinase 2b (p38 beta)	PF00069	26.087 (54/207)	1.44E-07
PAS domain-containing serine/threonine-protein kinase (PASK)	PF13426 ; PF00069	25.234 (54/214)	1.51E-07
Calmodulin-dependent kinase II (CAMKK2)	PF00069	23.353 (39/167)	1.58E-07
RAC-gamma serine/threonine-protein kinase (AKT3)	PF00169 ; PF00069 ; PF00433 More >>	24.121 (48/199)	1.82E-07
Polo-like kinase 1 (PLK1)	PF00069 ; PF00659	28.947 (44/152)	2.09E-07
Citron Rho-interacting kinase (CIT)	PF00780 ; PF00169 ; PF00069 More >>	23.810 (45/189)	2.15E-07
Doublecortin-like kinase 2 (DCLK2)	PF03607 ; PF00069	26.214 (54/206)	2.19E-07
Cyclin-dependent kinase-like 1 (CDKL1)	PF00069	23.267 (47/202)	2.63E-07
Stress-activated protein kinase JNK1 (JNK1)	PF00069	27.404 (57/208)	3.00E-07
Ribosomal protein S6 kinase-related protein (RSKR)	PF00069	34.940 (29/83)	3.31E-07
G protein-coupled receptor kinase 6 (GRK6)	PF00069 ; PF00615	24.638 (51/207)	3.40E-07
G protein-coupled receptor kinase 4 (GRK4)	PF00069 ; PF00615	26.066 (55/211)	3.50E-07
Obscurin (OBSCN)	PF00041 ; PF07679 ; PF00612 ; PF00069 ; PF00621 More >>	26.601 (54/203)	3.89E-07
Stress-activated protein kinase JNK2 (JNK2)	PF00069	27.805 (57/205)	4.18E-07
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (PHKG1)	PF00069	27.778 (60/216)	4.21E-07
RAC-beta serine/threonine-protein kinase (AKT2)	PF00169 ; PF00069 ; PF00433 More >>	23.645 (48/203)	4.21E-07
Serine/threonine-protein kinase pim-1 (PIM1)	PF00069	23.982 (53/221)	4.76E-07
Cyclin-dependent kinase-like 4 (CDKL4)	PF00069	22.059 (45/204)	5.33E-07
Serine/threonine-protein kinase H1 (PSKH1)	PF00069	24.878 (51/205)	6.12E-07
Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5)	PF00780 ; PF00069	23.636 (52/220)	6.13E-07
Cyclin-dependent kinase 11A (CDK11A)	PF00069	25.000 (51/204)	6.17E-07
Homeodomain-interacting protein kinase 4 (HIPK4)	PF00069	27.193 (62/228)	6.48E-07
TBC domain-containing protein kinase-like protein (TBCK)	PF00069 ; PF00566 ; PF00581 More >>	24.324 (45/185)	7.77E-07
Calcium/calmodulin-dependent protein kinase type II subunit delta (CAMK2D)	PF08332 ; PF00069	25.000 (53/212)	8.11E-07
Testis-specific serine/threonine-protein kinase 1 (TSSK1B)	PF00069	25.000 (53/212)	9.54E-07
Serine/threonine-protein kinase tousled-like 2 (TLK2)	PF00069	24.221 (70/289)	1.07E-06
G protein-coupled receptor kinase 5 (GRK5)	PF00069 ; PF00615	26.512 (57/215)	1.10E-06
Inhibitor of nuclear factor kappa-B kinase subunit epsilon (IKBKE)	PF00069 ; PF18394 ; PF18396 More >>	24.766 (53/214)	1.15E-06
Rhodopsin kinase GRK1 (GRK1)	PF00069 ; PF00615	34.375 (33/96)	1.16E-06
Endoplasmic reticulum to nucleus signaling 1 (ERN1)	PF00069 ; PF06479	28.251 (63/223)	1.17E-06
Protein kinase N3 (PKN3)	PF02185 ; PF00069 ; PF00433 More >>	25.306 (62/245)	1.27E-06
Cyclin-dependent kinase 10 (CDK10)	PF00069	25.463 (55/216)	1.28E-06
Bone morphogenetic protein receptor (BMPR2)	PF01064 ; PF00069	24.294 (86/354)	1.29E-06
Serine/threonine kinase-like domain-containing protein STKLD1 (STKLD1)	PF00069	23.529 (28/119)	1.31E-06
NF-kappa-B-activating kinase (TBK1)	PF00069 ; PF18394 ; PF18396 More >>	26.168 (56/214)	1.35E-06
Serine/threonine-protein kinase NIM1 (NIM1K)	PF00069	25.909 (57/220)	1.37E-06
Phosphorylase kinase testis gamma 2 (PHKG2)	PF00069	23.504 (55/234)	1.37E-06
Serine/threonine-protein kinase/endoribonuclease IRE2 (ERN2)	PF00069 ; PF06479	25.896 (65/251)	1.39E-06
Cyclin-dependent kinase-like 5 (CDKL5)	PF00069	24.000 (48/200)	1.70E-06
Mitogen-activated protein kinase 4 (MAPK4)	PF00069	23.005 (49/213)	1.79E-06
Cyclin-dependent kinase 11B (CDK11B)	PF00069	25.616 (52/203)	1.86E-06
Protein kinase N2 (PKN2)	PF02185 ; PF00069 ; PF00433 More >>	26.667 (64/240)	1.93E-06
PIM-3 protein kinase (PIM3)	PF00069	27.556 (62/225)	1.94E-06
TGF-beta-stimulated factor 1 (STK16)	PF00069	20.962 (61/291)	2.56E-06
RAC-alpha serine/threonine-protein kinase (AKT1)	PF00169 ; PF00069 ; PF00433 More >>	23.894 (54/226)	2.82E-06
Serine/threonine-protein kinase STK11 (STK11)	PF00069	22.674 (39/172)	2.91E-06
MEK kinase kinase 2 (MAP4K2)	PF00780 ; PF00069	23.618 (47/199)	3.07E-06
Serine/threonine-protein kinase 17B (STK17B)	PF00069	25.481 (53/208)	3.21E-06
NDR2 protein kinase (STK38L)	PF00069 ; PF00433	22.222 (74/333)	4.23E-06
Serine/threonine-protein kinase tousled-like 1 (TLK1)	PF00069	23.488 (66/281)	4.71E-06
Peripheral plasma membrane protein CASK (CASK)	PF00625 ; PF02828 ; PF00595 ; PF00069 ; PF00018 More >>	23.729 (56/236)	5.21E-06
MAPK/MAK/MRK overlapping kinase (MOK)	PF00069	21.256 (44/207)	5.37E-06
Cyclin-dependent kinase 19 (CDK19)	PF00069	27.273 (57/209)	5.98E-06
Calcium/calmodulin-dependent protein kinase type 1B (PNCK)	PF00069	23.875 (69/289)	7.26E-06
Aurora kinase B (AURKB)	PF00069	24.215 (54/223)	7.41E-06
Doublecortin-like kinase 3 (DCLK3)	PF00069	22.881 (54/236)	7.69E-06
Calcium/calmodulin-dependent protein kinase type 1D (CAMK1D)	PF00069	27.053 (56/207)	7.88E-06
TGF-beta receptor type I (TGFBR1)	PF01064 ; PF00069 ; PF08515 More >>	23.293 (58/249)	9.94E-06
Serine/threonine-protein kinase NIK (MAP3K14)	PF00069	27.513 (52/189)	1.10E-05
Rhodopsin kinase GRK7 (GRK7)	PF00069 ; PF00615	25.688 (56/218)	1.14E-05
Eukaryotic translation initiation factor 2-alpha kinase 4 (EIF2AK4)	PF12745 ; PF00069 ; PF05773 ; PF13393 More >>	26.797 (41/153)	1.26E-05
Inhibitor of nuclear factor kappa-B kinase alpha (IKKA)	PF18397 ; PF12179 ; PF00069 More >>	23.445 (49/209)	1.34E-05
Calcium/calmodulin-dependent protein kinase type II subunit gamma (CAMK2G)	PF08332 ; PF00069	23.113 (49/212)	1.41E-05
Anti-mullerian hormone II receptor (AMHR2)	PF00069	25.000 (41/164)	1.52E-05
Large tumor suppressor homolog 2 (LATS2)	PF00069 ; PF00433	20.561 (66/321)	1.55E-05
CaM-kinase IV kinase (CAMKK1)	PF00069	22.754 (38/167)	1.62E-05
Checkpoint kinase-1 (CHK1)	PF00069	25.359 (53/209)	1.89E-05
Serine/threonine-protein kinase SBK1 (SBK1)	PF00069	23.413 (59/252)	1.99E-05
Beta-adrenergic receptor kinase 1 (ADRBK1)	PF00169 ; PF00069 ; PF00615 More >>	24.651 (53/215)	2.33E-05
Doublecortin-like kinase 1 (DCLK1)	PF03607 ; PF00069	23.832 (51/214)	2.43E-05
Beta-adrenergic receptor kinase 2 (ADRBK2)	PF00169 ; PF00069 ; PF00615 More >>	24.651 (53/215)	2.45E-05
Activin receptor type IIA (ACVR2A)	PF01064 ; PF00069	21.918 (64/292)	2.70E-05
Eukaryotic translation initiation factor 2-alpha kinase 1 (EIF2AK1)	PF00069	31.132 (33/106)	3.05E-05
Casein kinase I alpha (CSNK1A1)	PF00069	26.144 (40/153)	3.07E-05
Protein kinase C epsilon (PRKCE)	PF00130 ; PF00168 ; PF00069 ; PF00433 More >>	22.222 (50/225)	3.55E-05
Polo-like kinase 2 (PLK2)	PF00069 ; PF00659	22.819 (34/149)	4.11E-05
Wee1-like protein kinase 2 (WEE2)	PF00069	26.056 (37/142)	4.47E-05
Rho-associated protein kinase 2 (ROCK2)	PF00069 ; PF08912	22.222 (48/216)	5.11E-05
STE20-related kinase adapter protein alpha (STRADA)	PF00069	21.304 (49/230)	5.57E-05
CDC42 binding protein kinase alpha (DMPK-like alpha)	PF00130 ; PF00780 ; PF08826 ; PF15796 ; PF00069 ; PF00433 More >>	23.810 (65/273)	6.72E-05
Cyclin-dependent kinase 8 (CDK8)	PF00069	34.375 (33/96)	7.77E-05
Activin receptor type IB (ACVR1B)	PF01064 ; PF00069 ; PF08515 More >>	23.695 (59/249)	8.96E-05
Extracellular matrix organizing protein FRAS1 (FRAS1)	PF16184 ; PF03160 ; PF00093 More >>	26.708 (43/161)	8.99E-05
Serine/threonine-protein kinase cot (COT)	PF00069	24.623 (49/199)	9.03E-05
Striated muscle preferentially expressed protein kinase (SPEG)	PF07679 ; PF00069 ; PF16650 More >>	25.833 (31/120)	9.20E-05
Rho-associated protein kinase 1 (ROCK1)	PF00069 ; PF08912	20.833 (45/216)	9.27E-05
Serine/threonine-protein kinase LATS1 (LATS1)	PF00069 ; PF00627	25.641 (40/156)	1.19E-04
Calcium/calmodulin-dependent protein kinase type II subunit alpha (CAMK2A)	PF08332 ; PF00069	24.528 (52/212)	1.30E-04
Wee1-like protein kinase (WEE1)	PF00069	23.592 (67/284)	1.43E-04
Casein kinase I isoform alpha-like (CSNK1A1L)	PF00069	26.144 (40/153)	1.54E-04
Testis-specific serine/threonine-protein kinase 3 (TSSK3)	PF00069	26.531 (39/147)	1.60E-04
Serine/threonine-protein kinase SBK2 (SBK2)	PF00069	27.419 (51/186)	1.66E-04
Activin receptor type IIB (ACVR2B)	PF01064 ; PF00069	22.477 (49/218)	2.57E-04
MAPK-activated protein kinase 3 (MAPKAPK3)	PF00069	25.751 (60/233)	3.76E-04
Kalirin (KALRN)	PF13716 ; PF00041 ; PF07679 ; PF00169 ; PF00069 ; PF00621 ; PF16609 ; PF00435 More >>	24.171 (51/211)	4.27E-04
Serine/threonine-protein kinase MRCK gamma (CDC42BPG)	PF00130 ; PF00780 ; PF08826 ; PF00069 More >>	24.771 (54/218)	4.78E-04
Casein kinase I gamma-2 (CSNK1G2)	PF12605 ; PF00069	23.684 (54/228)	5.53E-04
Tau-tubulin kinase 2 (TTBK2)	PF00069	22.034 (52/236)	5.63E-04
Casein kinase I gamma-3 (CSNK1G3)	PF12605 ; PF00069	22.807 (52/228)	5.69E-04
Serine/threonine-protein kinase 35 (STK35)	PF00069	21.583 (60/278)	6.06E-04
Serine/threonine-protein kinase ULK4 (ULK4)	PF00069	24.171 (51/211)	6.37E-04
Casein kinase I delta (CSNK1D)	PF00069	24.681 (58/235)	7.23E-04
CaM kinase-like vesicle-associated protein (CAMKV)	PF00069	24.309 (44/181)	7.81E-04
Dual-specificity tyrosine-phosphorylation regulated kinase 3 (DYRK3)	PF00069	21.569 (44/204)	8.95E-04
Casein kinase I epsilon (CSNK1E)	PF00069	23.750 (57/240)	1.00E-03
MAP kinase signal-integrating kinase 2 (MKNK2)	PF00069	27.211 (40/147)	1.00E-03
Calcium/calmodulin-dependent protein kinase type II subunit beta (CAMK2B)	PF08332 ; PF00069	23.005 (49/213)	1.00E-03
Homeodomain interacting protein kinase 2 (HIPK2)	PF00069	23.984 (59/246)	3.00E-03
IL-1 receptor-associated kinase 3 (IRAK3)	PF00531 ; PF00069	22.066 (47/213)	4.00E-03
Serine/threonine-protein kinase 40 (STK40)	PF00069	26.241 (37/141)	4.00E-03
Homeodomain-interacting protein kinase 1 (HIPK1)	PF00069	25.161 (39/155)	4.00E-03
Serine/threonine-protein kinase PDIK1L (PDIK1L)	PF00069	20.543 (53/258)	5.00E-03
Membrane-associated kinase (PKMYT1)	PF00069	22.381 (47/210)	5.00E-03
Homeodomain-interacting protein kinase 3 (HIPK3)	PF00069	20.352 (81/398)	5.00E-03
Tau-tubulin kinase (TTBK1)	PF00069	22.414 (52/232)	5.00E-03
Triple functional domain protein (TRIO)	PF00650 ; PF07679 ; PF00169 ; PF00069 ; PF00621 ; PF16609 ; PF00018 ; PF00435 More >>	25.000 (52/208)	5.00E-03
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Note: If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.

KEGG Pathway	Pathway ID	Affiliated Target
MAPK signaling pathway	hsa04010	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
ErbB signaling pathway	hsa04012	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Ras signaling pathway	hsa04014	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Rap1 signaling pathway	hsa04015	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Calcium signaling pathway	hsa04020	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
HIF-1 signaling pathway	hsa04066	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
FoxO signaling pathway	hsa04068	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Phospholipase D signaling pathway	hsa04072	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Endocytosis	hsa04144	Affiliated Target
Class: Cellular Processes => Transport and catabolism	Pathway Hierarchy
PI3K-Akt signaling pathway	hsa04151	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Focal adhesion	hsa04510	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
Adherens junction	hsa04520	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
Gap junction	hsa04540	Affiliated Target
Class: Cellular Processes => Cellular community - eukaryotes	Pathway Hierarchy
JAK-STAT signaling pathway	hsa04630	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Regulation of actin cytoskeleton	hsa04810	Affiliated Target
Class: Cellular Processes => Cell motility	Pathway Hierarchy
GnRH signaling pathway	hsa04912	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Estrogen signaling pathway	hsa04915	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Oxytocin signaling pathway	hsa04921	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Relaxin signaling pathway	hsa04926	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Parathyroid hormone synthesis, secretion and action	hsa04928	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
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Degree	137	Degree centrality	1.47E-02	Betweenness centrality	2.54E-02
Closeness centrality	2.82E-01	Radiality	1.48E+01	Clustering coefficient	6.91E-02
Neighborhood connectivity	3.41E+01	Topological coefficient	2.04E-02	Eccentricity	11
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Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target Regulators

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Target-regulating microRNAs

Target-regulating microRNAs Info

Target-regulating Transcription Factors

Target-regulating Transcription Factors Info

Target-interacting Proteins

Target-interacting Proteins Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Drug Resistance
Mutation (DRM)

Drug Resistance Mutation Info

Target Affiliated Biological Pathways		Top
KEGG Pathway	[+] 32 KEGG Pathways	+
1	MAPK signaling pathway
2	ErbB signaling pathway
3	Ras signaling pathway
4	Rap1 signaling pathway
5	Calcium signaling pathway
6	Cytokine-cytokine receptor interaction
7	HIF-1 signaling pathway
8	FoxO signaling pathway
9	Endocytosis
10	PI3K-Akt signaling pathway
11	Dorso-ventral axis formation
12	Focal adhesion
13	Adherens junction
14	Gap junction
15	Regulation of actin cytoskeleton
16	GnRH signaling pathway
17	Estrogen signaling pathway
18	Oxytocin signaling pathway
19	Epithelial cell signaling in Helicobacter pylori infection
20	Hepatitis C
21	Pathways in cancer
22	Proteoglycans in cancer
23	MicroRNAs in cancer
24	Pancreatic cancer
25	Endometrial cancer
26	Glioma
27	Prostate cancer
28	Melanoma
29	Bladder cancer
30	Non-small cell lung cancer
31	Central carbon metabolism in cancer
32	Choline metabolism in cancer
NetPath Pathway	[+] 2 NetPath Pathways	+
1	IL4 Signaling Pathway
2	EGFR1 Signaling Pathway
Panther Pathway	[+] 2 Panther Pathways	+
1	Cadherin signaling pathway
2	EGF receptor signaling pathway
PID Pathway	[+] 19 PID Pathways	+
1	LPA receptor mediated events
2	Signaling events mediated by PTP1B
3	Arf6 signaling events
4	Signaling events mediated by TCPTP
5	Thromboxane A2 receptor signaling
6	SHP2 signaling
7	Regulation of Telomerase
8	EGF receptor (ErbB1) signaling pathway
9	EGFR-dependent Endothelin signaling events
10	Posttranslational regulation of adherens junction stability and dissassembly
11	Direct p53 effectors
12	ErbB1 downstream signaling
13	Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling
14	E-cadherin signaling in keratinocytes
15	ErbB receptor signaling network
16	Internalization of ErbB1
17	Stabilization and expansion of the E-cadherin adherens junction
18	a6b1 and a6b4 Integrin signaling
19	Syndecan-3-mediated signaling events
Reactome	[+] 14 Reactome Pathways	+
1	Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
2	SHC1 events in ERBB2 signaling
3	PLCG1 events in ERBB2 signaling
4	PIP3 activates AKT signaling
5	GRB2 events in EGFR signaling
6	GAB1 signalosome
7	SHC1 events in EGFR signaling
8	EGFR downregulation
9	GRB2 events in ERBB2 signaling
10	PI3K events in ERBB2 signaling
11	EGFR Transactivation by Gastrin
12	Constitutive Signaling by Aberrant PI3K in Cancer
13	Constitutive Signaling by EGFRvIII
14	RAF/MAP kinase cascade
WikiPathways	[+] 29 WikiPathways	+
1	ErbB Signaling Pathway
2	Regulation of Actin Cytoskeleton
3	EGF/EGFR Signaling Pathway
4	MAPK Signaling Pathway
5	Focal Adhesion
6	Aryl Hydrocarbon Receptor Pathway
7	Extracellular vesicle-mediated signaling in recipient cells
8	TCA Cycle Nutrient Utilization and Invasiveness of Ovarian Cancer
9	Hair Follicle Development: Cytodifferentiation (Part 3 of 3)
10	Bladder Cancer
11	Hair Follicle Development: Induction (Part 1 of 3)
12	Signaling by ERBB4
13	Signaling by ERBB2
14	Gastrin-CREB signalling pathway via PKC and MAPK
15	PIP3 activates AKT signaling
16	Nanoparticle-mediated activation of receptor signaling
17	Aryl Hydrocarbon Receptor
18	Spinal Cord Injury
19	Integrated Pancreatic Cancer Pathway
20	Gastric cancer network 2
21	AGE/RAGE pathway
22	Signaling Pathways in Glioblastoma
23	Arylhydrocarbon receptor (AhR) signaling pathway
24	miR-targeted genes in muscle cell - TarBase
25	miR-targeted genes in lymphocytes - TarBase
26	miR-targeted genes in epithelium - TarBase
27	Integrated Breast Cancer Pathway
28	Signaling by EGFR
29	L1CAM interactions

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

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