Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T46781 Target Info
Target Name Aurora kinase B (AURKB)
Synonyms Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
Target Type Clinical trial Target
Gene Name AURKB
Biochemical Class Kinase
UniProt ID
AURKB_HUMAN
Co-Targets of This Target  Top
Co-Target Name Platelet-derived growth factor receptor alpha (PDGFRA) Successful Target
UniProt ID PGFRA_HUMAN
Gene Name PDGFRA
Synonyms RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor
Representative Drug(s) ABT-348 Drug Info Ki = 0.7943 nM Click to Show More [1]
2 AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Fibroblast growth factor receptor 2 (FGFR2) Successful Target
UniProt ID FGFR2_HUMAN
Gene Name FGFR2
Synonyms Keratinocyte growth factor receptor 2; Keratinocyte growth factor receptor; KSAM; KGFR; K-sam; FGFR-2; FGF-2 receptor; CD332; BEK
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms Tyrosine-protein kinase JAK2
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [3]
Co-Target Name Janus kinase 3 (JAK-3) Successful Target
UniProt ID JAK3_HUMAN
Gene Name JAK3
Synonyms Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [3]
Co-Target Name Proto-oncogene c-Ret (RET) Successful Target
UniProt ID RET_HUMAN
Gene Name RET
Synonyms RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM Click to Show More [2]
2 ABT-348 Drug Info IC50 = 7 nM [5]
3 PHA-739358 Drug Info IC50 = 31 nM [9]
Co-Target Name Vascular endothelial growth factor receptor 2 (KDR) Successful Target
UniProt ID VGFR2_HUMAN
Gene Name KDR
Synonyms VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
Representative Drug(s) ABT-348 Drug Info IC50 = 2 nM Click to Show More [4]
2 AT9283 Drug Info IC50 = 10 nM [2]
3 R763 Drug Info IC50 = 19 nM [4]
4 CYC116 Drug Info Ki = 44 nM [10]
5 Rosiglitazone + metformin Drug Info IC50 = 135 nM [14]
6 PHA-739358 Drug Info IC50 = 432 nM [9]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
Representative Drug(s) ABT-348 Drug Info IC50 = 3 nM Click to Show More [5]
2 VX-680 Drug Info Ki = 80 nM [3]
3 PHA-739358 Drug Info IC50 = 155 nM [9]
4 AZD-1152-HQPA Drug Info Ki = 170 nM [15]
Co-Target Name Platelet-derived growth factor receptor beta (PDGFRB) Successful Target
UniProt ID PGFRB_HUMAN
Gene Name PDGFRB
Synonyms Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor
Representative Drug(s) ABT-348 Drug Info IC50 = 3 nM Click to Show More [5]
2 Rosiglitazone + metformin Drug Info IC50 = 50 nM [11]
Co-Target Name Tyrosine-protein kinase ABL1 (ABL) Successful Target
UniProt ID ABL1_HUMAN
Gene Name ABL1
Synonyms p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
Representative Drug(s) AT9283 Drug Info IC50 = 4 nM Click to Show More [3]
2 PHA-739358 Drug Info IC50 = 5 nM [6]
3 ABT-348 Drug Info IC50 = 12 nM [5]
4 VX-680 Drug Info Ki = 30 nM [3]
Co-Target Name Fibroblast growth factor receptor 1 (FGFR1) Successful Target
UniProt ID FGFR1_HUMAN
Gene Name FGFR1
Synonyms c-fgr; bFGF-R-1; bFGF-R; N-sam; HBGFR; Fms-like tyrosine kinase 2; FLT2; FLT-2; FLG; FGFR-1; FGFBR; CEK; CD331 antigen; CD331; Basic fibroblast growth factor receptor 1; BFGFR
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM Click to Show More [2]
2 PHA-739358 Drug Info IC50 = 47 nM [9]
3 GSK1070916 Drug Info IC50 = 76 nM [13]
4 ABT-348 Drug Info IC50 = 188 nM [5]
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM Click to Show More [2]
2 CYC116 Drug Info IC50 = 25.12 nM [7]
3 VX-680 Drug Info IC50 = 30 nM [8]
4 AZD-1152-HQPA Drug Info IC50 = 100 nM [7]
5 PHA-739358 Drug Info IC50 = 669 nM [9]
Co-Target Name Proto-oncogene c-Src (SRC) Successful Target
UniProt ID SRC_HUMAN
Gene Name SRC
Synonyms pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM Click to Show More [2]
2 CYC116 Drug Info Ki = 820 nM [10]
Co-Target Name Tropomyosin-related kinase A (TrkA) Successful Target
UniProt ID NTRK1_HUMAN
Gene Name NTRK1
Synonyms gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
Representative Drug(s) PHA-739358 Drug Info IC50 = 30 nM [9]
Co-Target Name Fusion protein Bcr-Abl (Bcr-Abl) Successful Target
UniProt ID BCR_HUMAN-ABL1_HUMAN
Gene Name BCR-ABL1
Synonyms BCR-ABL fusion protein; BCR-ABL
Representative Drug(s) VX-680 Drug Info IC50 = 50.12 nM [12]
Co-Target Name Fyn tyrosine protein kinase (FYN) Successful Target
UniProt ID FYN_HUMAN
Gene Name FYN
Synonyms Tyrosine-protein kinase Fyn; Src-like kinase; SLK; Proto-oncogene tyrosine-protein kinase Fyn; Proto-oncogene c-Fyn; Proto-oncogene Syn; Fyn p59-Fyn; Fyn Protooncogene Syn
Representative Drug(s) ABT-348 Drug Info IC50 = 110 nM [5]
Co-Target Name ALK tyrosine kinase receptor (ALK) Successful Target
UniProt ID ALK_HUMAN
Gene Name ALK
Synonyms CD246; Anaplastic lymphoma kinase
Representative Drug(s) ABT-348 Drug Info IC50 = 363 nM [5]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
Representative Drug(s) PHA-739358 Drug Info IC50 = 407 nM [9]
Co-Target Name Rho-associated protein kinase 1 (ROCK1) Successful Target
UniProt ID ROCK1_HUMAN
Gene Name ROCK1
Synonyms Rok; Rho-associated, coiled-coil containing protein kinase 1; Rho-associated kinase 1; Rho kinase; ROCK1; ROCK; P160ROCK; P160(rock); P160 ROCK-1; Let-502 kinase
Representative Drug(s) ABT-348 Drug Info IC50 = 456 nM [5]
Co-Target Name Insulin-like growth factor I receptor (IGF1R) Successful Target
UniProt ID IGF1R_HUMAN
Gene Name IGF1R
Synonyms Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221
Representative Drug(s) ABT-348 Drug Info IC50 = 539 nM [5]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
Representative Drug(s) ABT-348 Drug Info IC50 = 1000 nM [5]
Co-Target Name Aurora kinase A (AURKA) Clinical trial Target
UniProt ID AURKA_HUMAN
Gene Name AURKA
Synonyms hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
Representative Drug(s) MK-5108 Drug Info IC50 = 0.046 nM Click to Show More [16]
2 VX-680 Drug Info IC50 = 0.24 nM [17]
3 PHA-739358 Drug Info Ki = 2.5 nM [9]
4 AT9283 Drug Info IC50 = 3 nM [3]
5 AMG 900 Drug Info IC50 = 5 nM [18]
6 CYC116 Drug Info Ki = 8 nM [10]
7 ABT-348 Drug Info IC50 = 12 nM [5]
8 GSK1070916 Drug Info Ki = 490 nM [13]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM Click to Show More [2]
2 GSK1070916 Drug Info IC50 = 74 nM [13]
3 PHA-739358 Drug Info IC50 = 161 nM [9]
Co-Target Name Glycogen synthase kinase-3 beta (GSK-3B) Clinical trial Target
UniProt ID GSK3B_HUMAN
Gene Name GSK3B
Synonyms Serine/threonine-protein kinase GSK3B; GSK-3 beta
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Aurora kinase C (AURKC) Clinical trial Target
UniProt ID AURKC_HUMAN
Gene Name AURKC
Synonyms Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
Representative Drug(s) AMG 900 Drug Info IC50 = 1 nM Click to Show More [18]
2 GSK1070916 Drug Info Ki = 1.5 nM [13]
3 VX-680 Drug Info IC50 = 4.6 nM [19]
4 MK-5108 Drug Info IC50 = 12 nM [16]
5 AZD-1152-HQPA Drug Info Ki = 17 nM [15]
6 PHA-739358 Drug Info IC50 = 61 nM [9]
7 CYC116 Drug Info IC50 = 65 nM [3]
8 Rosiglitazone + metformin Drug Info IC50 = 210 nM [22]
Co-Target Name TYK2 tyrosine kinase (TYK2) Clinical trial Target
UniProt ID TYK2_HUMAN
Gene Name TYK2
Synonyms Non-receptor tyrosine-protein kinase TYK2
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Yes tyrosine kinase (YES) Clinical trial Target
UniProt ID YES_HUMAN
Gene Name YES1
Synonyms p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Tyrosine-protein kinase Mer (MERTK) Clinical trial Target
UniProt ID MERTK_HUMAN
Gene Name MERTK
Synonyms Receptor tyrosine kinase MerTK; Proto-oncogene c-Mer
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Macrophage colony-stimulating factor 1 receptor (CSF1R) Clinical trial Target
UniProt ID CSF1R_HUMAN
Gene Name CSF1R
Synonyms Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
Representative Drug(s) ABT-348 Drug Info Ki = 3.162 nM [1]
Co-Target Name Fibroblast growth factor receptor 3 (FGFR3) Clinical trial Target
UniProt ID FGFR3_HUMAN
Gene Name FGFR3
Synonyms JTK4; FGFR-3; CD333
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Vascular endothelial growth factor receptor 1 (FLT-1) Clinical trial Target
UniProt ID VGFR1_HUMAN
Gene Name FLT1
Synonyms Vascular permeability factor receptor; VEGFR1; VEGFR-1; VEGF-1 receptor; Tyrosine-protein kinase receptor FLT; Tyrosine-protein kinase FRT; Fms-like tyrosine kinase 1; FRT; FLT
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM Click to Show More [2]
2 Rosiglitazone + metformin Drug Info IC50 = 28 nM [14]
3 ABT-348 Drug Info IC50 = 32 nM [5]
4 GSK1070916 Drug Info IC50 = 42 nM [13]
Co-Target Name Protein delta homolog 1 (DLK1) Clinical trial Target
UniProt ID DLK1_HUMAN
Gene Name DLK1
Synonyms pG2; DLK-1
Representative Drug(s) VX-680 Drug Info Ki = 35.8 nM [20]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name TEK
Synonyms hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b
Representative Drug(s) GSK1070916 Drug Info IC50 = 59 nM [13]
Co-Target Name Receptor-interacting protein 1 (RIPK1) Clinical trial Target
UniProt ID RIPK1_HUMAN
Gene Name RIPK1
Synonyms Receptor-interacting serine/threonine-protein kinase 1; RIP1; RIP-1; RIP; Cell death protein RIP
Representative Drug(s) VX-680 Drug Info IC50 = 208 nM [21]
Co-Target Name Cyclin-dependent kinase 2 (CDK2) Clinical trial Target
UniProt ID CDK2_HUMAN
Gene Name CDK2
Synonyms Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
Representative Drug(s) CYC116 Drug Info Ki = 390 nM Click to Show More [10]
2 PHA-739358 Drug Info IC50 = 462 nM [9]
Co-Target Name Maternal embryonic leucine zipper kinase (MELK) Clinical trial Target
UniProt ID MELK_HUMAN
Gene Name MELK
Synonyms Protein kinase PK38; Protein kinase Eg3
Representative Drug(s) VX-680 Drug Info IC50 = 420 nM Click to Show More [22]
2 AT9283 Drug Info IC50 = 685 nM [23]
Co-Target Name Cyclin-dependent kinase 9 (CDK9) Clinical trial Target
UniProt ID CDK9_HUMAN
Gene Name CDK9
Synonyms Tat-associated kinase complex catalytic subunit; TAK; Similar to cyclin-dependent kinase 9; Serine/threonine-protein kinase PITALRE; Cyclin-dependent protein kinase Cdk9; Cell division protein kinase 9; Cell division cycle 2-like protein kinase 4; CDC2L4; CDC2-related kinase; C-2K
Representative Drug(s) CYC116 Drug Info Ki = 480 nM [10]
Co-Target Name Positive transcription elongation factor b (P-TEFb) Clinical trial Target
UniProt ID CDK9_HUMAN-CCNT1_HUMAN
Gene Name CDK9-CCNT1
Synonyms P-TEFb
Representative Drug(s) CYC116 Drug Info Ki = 480 nM [10]
Co-Target Name Ribosomal protein S6 kinase beta-1 (S6K1) Clinical trial Target
UniProt ID KS6B1_HUMAN
Gene Name RPS6KB1
Synonyms p70-S6K 1; p70 ribosomal S6 kinase alpha; p70 S6KA; p70 S6K-alpha; p70 S6 kinase alpha; Serine/threonine-protein kinase 14A; STK14A; S6K-beta-1; S6K; Ribosomal protein S6 kinase I; P70S6K1; P70-S6K; 70 kDa ribosomal protein S6 kinase 1
Representative Drug(s) CYC116 Drug Info Ki = 540 nM [10]
Co-Target Name Ribosomal protein S6 kinase alpha-3 (RSK3) Patented-recorded Target
UniProt ID KS6A3_HUMAN
Gene Name RPS6KA3
Synonyms pp90RSK2; p90RSK3; p90-RSK 3; S6K-alpha-3; Ribosomal S6 kinase 2; RSK2; RSK-2; MAPKAPK1B; MAPKAPK-1b; MAPKAP kinase 1b; MAPK-activated protein kinase 1b; MAP kinase-activated protein kinase 1b; Insulin-stimulated protein kinase 1; ISPK1; ISPK-1; 90 kDa ribosomal protein S6 kinase 3
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name NF-kappa-B-activating kinase (TBK1) Patented-recorded Target
UniProt ID TBK1_HUMAN
Gene Name TBK1
Synonyms TANK-binding kinase 1; T2K; Serine/threonine-protein kinase TBK1; NAK
Representative Drug(s) VX-680 Drug Info IC50 = 6.22 nM [24]
Co-Target Name Pyruvate dehydrogenase kinase 1 (PDHK1) Patented-recorded Target
UniProt ID PDK1_HUMAN
Gene Name PDK1
Synonyms Pyruvate dehydrogenase kinase isoform 1; Pyruvate dehydrogenase (acetyl-transferring) kinase isozyme 1, mitochondrial; PDHK1; PDH kinase 1
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Discoidin domain-containing receptor 2 (DDR2) Patented-recorded Target
UniProt ID DDR2_HUMAN
Gene Name DDR2
Synonyms Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B
Representative Drug(s) VX-680 Drug Info IC50 = 18 nM [25]
Co-Target Name Ribosomal protein S6 kinase alpha-2 (RSK2) Literature-reported Target
UniProt ID KS6A2_HUMAN
Gene Name RPS6KA2
Synonyms pp90RSK3; p90RSK2; p90-RSK 2; S6K-alpha-2; Ribosomal S6 kinase 3; RSK3; RSK-3; MAPKAPK1C; MAPKAPK-1c; MAPKAP kinase 1c; MAPK-activated protein kinase 1c; MAP kinase-activated protein kinase 1c; 90 kDa ribosomal protein S6 kinase 2
Representative Drug(s) AT9283 Drug Info IC50 = 1 nM [2]
Co-Target Name Protein kinase D (PRKD1) Literature-reported Target
UniProt ID KPCD1_HUMAN
Gene Name PRKD1
Synonyms nPKC-mu; nPKC-D1; Serine/threonine-protein kinase D1; Protein kinase C mu type; PRKCM; PKD1; PKD
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Cytoplasmic DRAK1 (STK17A) Literature-reported Target
UniProt ID ST17A_HUMAN
Gene Name STK17A
Synonyms Serine/threonine-protein kinase 17A; STK17A; DAP kinase-related apoptosis-inducing protein kinase 1
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Polo-like kinase 4 (PLK4) Literature-reported Target
UniProt ID PLK4_HUMAN
Gene Name PLK4
Synonyms Serine/threonine-protein kinase Sak; Serine/threonine-protein kinase PLK4; Serine/threonine-protein kinase 18; STK18; SAK; PLK-4
Representative Drug(s) VX-680 Drug Info Ki = 11 nM [26]
Co-Target Name Salt-inducible kinase 1 (SIK1) Literature-reported Target
UniProt ID SIK1_HUMAN
Gene Name SIK1
Synonyms Serine/threonine-protein kinase SNF1LK; Serine/threonine-protein kinase SNF1-like kinase 1; Serine/threonine-protein kinase SIK1; SNF1LK; SIK-1; SIK
Representative Drug(s) GSK1070916 Drug Info IC50 = 70 nM [13]
Co-Target Name STE20-related serine/threonine-protein kinase (SLK) Literature-reported Target
UniProt ID SLK_HUMAN
Gene Name SLK
Synonyms hSLK; STE20-related kinase; STE20-like kinase
Representative Drug(s) PHA-739358 Drug Info IC50 = 621 nM [9]
Co-Target Name Aurora kinase A-interacting protein (AURKAIP1) Co-Target
UniProt ID AKIP_HUMAN
Gene Name AURKAIP1
Synonyms Mitochondrial small ribosomal subunit protein mS38; AURKA-interacting protein; 28S ribosomal protein S38, mitochondrial; MRP-S38
Representative Drug(s) VX-680 Drug Info Ki = 0.6 nM [8]
Co-Target Name Aurora kinase C-Inner centromere protein complex (AURKC-INCENP) Co-Target
UniProt ID AURKC_HUMAN-INCE_HUMAN
Gene Name AURKC-INCENP
Representative Drug(s) GSK1070916 Drug Info Ki = 1.5 nM [18]
Co-Target Name Ribosomal protein S6 kinase alpha 4 (RPS6KA4) Co-Target
UniProt ID KS6A4_HUMAN
Gene Name RPS6KA4
Synonyms Ribosomal protein S6 kinase alpha-4; S6K-alpha-4; 90 kDa ribosomal protein S6 kinase 4; Nuclear mitogen- and stress-activated protein kinase 2; Ribosomal protein kinase B; RSKB
Representative Drug(s) AT9283 Drug Info IC50 = 10 nM [2]
Co-Target Name Aurora kinase A-Targeting protein for Xklp2 complex (AURKA-TPX2) Co-Target
UniProt ID AURKA_HUMAN-TPX2_HUMAN
Gene Name AURKA-TPX2
Representative Drug(s) TAK-901 Drug Info IC50 = 21 nM Click to Show More [18]
2 GSK1070916 Drug Info Ki = 490 nM [18]
Co-Target Name Cyclin dependent kinase 2-G1/S specific cyclin E1 complex (CDK2-CCNE1) Co-Target
UniProt ID CDK2_HUMAN-CCNE1_HUMAN
Gene Name CDK2-CCNE1
Representative Drug(s) CYC116 Drug Info Ki = 390 nM [10]
References  Top
REF 1 Targeted kinase selectivity from kinase profiling data. ACS Med Chem Lett. 2012 Mar 14;3(5):383-6.
REF 2 Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J Med Chem. 2009 Jan 22;52(2):379-88.
REF 3 Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.
REF 4 Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5.
REF 5 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12.
REF 6 A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl. J Med Chem. 2010 Aug 12;53(15):5439-48.
REF 7 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 8 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41.
REF 9 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem. 2006 Nov 30;49(24):7247-51.
REF 10 Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. J Med Chem. 2010 Jun 10;53(11):4367-78.
REF 11 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases. Bioorg Med Chem Lett. 2009 Feb 1;19(3):745-50.
REF 12 BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2442-50.
REF 13 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001.
REF 14 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
REF 15 Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J Med Chem. 2007 May 3;50(9):2213-24.
REF 16 Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design. Eur J Med Chem. 2016 Nov 29;124:186-99.
REF 17 Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7392-7416.
REF 18 A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies. Eur J Med Chem. 2017 Nov 10;140:1-19.
REF 19 SAR156497, an exquisitely selective inhibitor of aurora kinases. J Med Chem. 2015 Jan 8;58(1):362-75.
REF 20 Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-87.
REF 21 Tozasertib Analogues as Inhibitors of Necroptotic Cell Death. J Med Chem. 2018 Mar 8;61(5):1895-920.
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