Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T87675 | Target Info | |||
| Target Name | Aurora kinase A (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
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| Target Type | Clinical trial Target | ||||
| Gene Name | AURKA | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | Ki = 0.7943 nM | Click to Show More | [1] | |
| 2 | AT9283 | Drug Info | IC50 = 10 nM | [2] | ||
| 3 | ENMD-2076 | Drug Info | IC50 = 10 nM | [4] | ||
| 4 | MLN8054 | Drug Info | IC50 = 794.33 nM | [8] | ||
| 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
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| 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
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| 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
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| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 1 nM | Click to Show More | [2] | |
| 2 | ABT-348 | Drug Info | IC50 = 7 nM | [6] | ||
| 3 | ENMD-2076 | Drug Info | IC50 = 10 nM | [4] | ||
| 4 | PHA-739358 | Drug Info | IC50 = 31 nM | [10] | ||
| 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
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| Representative Drug(s) | ENMD-2076 | Drug Info | IC50 = 1.86 nM | Click to Show More | [4] | |
| 2 | AT9283 | Drug Info | IC50 = 10 nM | [2] | ||
| 3 | CYC116 | Drug Info | IC50 = 25.12 nM | [8] | ||
| 4 | VX-680 | Drug Info | IC50 = 30 nM | [9] | ||
| 5 | PHA-739358 | Drug Info | IC50 = 669 nM | [10] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 2 nM | Click to Show More | [5] | |
| 2 | AT9283 | Drug Info | IC50 = 10 nM | [2] | ||
| 3 | ENMD-2076 | Drug Info | IC50 = 10 nM | [4] | ||
| 4 | R763 | Drug Info | IC50 = 19 nM | [5] | ||
| 5 | CYC116 | Drug Info | Ki = 44 nM | [11] | ||
| 6 | Rosiglitazone + metformin | Drug Info | IC50 = 135 nM | [14] | ||
| 7 | PHA-739358 | Drug Info | IC50 = 432 nM | [10] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 3 nM | Click to Show More | [6] | |
| 2 | VX-680 | Drug Info | Ki = 80 nM | [3] | ||
| 3 | PHA-739358 | Drug Info | IC50 = 155 nM | [10] | ||
| 4 | MLN8237 | Drug Info | IC50 = 320 nM | [3] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 3 nM | Click to Show More | [6] | |
| 2 | Rosiglitazone + metformin | Drug Info | IC50 = 50 nM | [12] | ||
| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 4 nM | Click to Show More | [3] | |
| 2 | PHA-739358 | Drug Info | IC50 = 5 nM | [7] | ||
| 3 | ABT-348 | Drug Info | IC50 = 12 nM | [6] | ||
| 4 | VX-680 | Drug Info | Ki = 30 nM | [3] | ||
| 5 | ENMD-2076 | Drug Info | IC50 = 81 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 10 nM | Click to Show More | [2] | |
| 2 | PHA-739358 | Drug Info | IC50 = 47 nM | [10] | ||
| 3 | ENMD-2076 | Drug Info | IC50 = 93 nM | [3] | ||
| 4 | ABT-348 | Drug Info | IC50 = 188 nM | [6] | ||
| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 10 nM | Click to Show More | [2] | |
| 2 | ENMD-2076 | Drug Info | IC50 = 10 nM | [4] | ||
| 3 | CYC116 | Drug Info | Ki = 820 nM | [11] | ||
| 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
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| Representative Drug(s) | PHA-739358 | Drug Info | IC50 = 30 nM | [10] | ||
| 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
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| Representative Drug(s) | VX-680 | Drug Info | IC50 = 50.12 nM | [13] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 110 nM | [6] | ||
| 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
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| Representative Drug(s) | ENMD-2076 | Drug Info | IC50 = 120 nM | Click to Show More | [3] | |
| 2 | PHA-739358 | Drug Info | IC50 = 407 nM | [10] | ||
| Co-Target Name | GABA(A) receptor alpha-1 (GABRA1) | Successful Target | ||||
| UniProt ID | GBRA1_HUMAN | |||||
| Gene Name | GABRA1 | |||||
| Synonyms |
Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1
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| Representative Drug(s) | MLN8054 | Drug Info | IC50 = 330 nM | Click to Show More | [15] | |
| 2 | MLN8237 | Drug Info | IC50 = 490 nM | [15] | ||
| Co-Target Name | ALK tyrosine kinase receptor (ALK) | Successful Target | ||||
| UniProt ID | ALK_HUMAN | |||||
| Gene Name | ALK | |||||
| Synonyms |
CD246; Anaplastic lymphoma kinase
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 363 nM | [6] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 456 nM | [6] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 539 nM | [6] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | IC50 = 1000 nM | [6] | ||
| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 1 nM | Click to Show More | [2] | |
| 2 | PHA-739358 | Drug Info | IC50 = 161 nM | [10] | ||
| 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
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| 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
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| Representative Drug(s) | AMG 900 | Drug Info | IC50 = 1 nM | Click to Show More | [16] | |
| 2 | VX-680 | Drug Info | IC50 = 4.6 nM | [20] | ||
| 3 | MK-5108 | Drug Info | IC50 = 12 nM | [22] | ||
| 4 | PHA-739358 | Drug Info | IC50 = 61 nM | [10] | ||
| 5 | CYC116 | Drug Info | IC50 = 65 nM | [3] | ||
| 6 | Rosiglitazone + metformin | Drug Info | IC50 = 210 nM | [23] | ||
| Co-Target Name | TYK2 tyrosine kinase (TYK2) | Successful Target | ||||
| UniProt ID | TYK2_HUMAN | |||||
| Gene Name | TYK2 | |||||
| Synonyms |
Non-receptor tyrosine-protein kinase TYK2
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| 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
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| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 1 nM | [2] | ||
| Co-Target Name | Aurora kinase B (AURKB) | Clinical trial Target | ||||
| UniProt ID | AURKB_HUMAN | |||||
| Gene Name | 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
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| Representative Drug(s) | MLN8237 | Drug Info | IC50 = 1.5 nM | Click to Show More | [17] | |
| 2 | VX-680 | Drug Info | Ki = 1.8 nM | [18] | ||
| 3 | ABT-348 | Drug Info | IC50 = 2 nM | [6] | ||
| 4 | AT9283 | Drug Info | IC50 = 2.7 nM | [19] | ||
| 5 | AMG 900 | Drug Info | IC50 = 4 nM | [16] | ||
| 6 | CYC116 | Drug Info | Ki = 9.2 nM | [11] | ||
| 7 | MLN8054 | Drug Info | IC50 = 9.3 nM | [21] | ||
| 8 | MK-5108 | Drug Info | IC50 ~ 10 nM | [17] | ||
| 9 | Rosiglitazone + metformin | Drug Info | IC50 = 35 nM | [23] | ||
| 10 | R763 | Drug Info | IC50 = 54 nM | [5] | ||
| 11 | PHA-739358 | Drug Info | IC50 = 79 nM | [3] | ||
| 12 | ENMD-2076 | Drug Info | IC50 = 290 nM | [26] | ||
| 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
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| Representative Drug(s) | ABT-348 | Drug Info | Ki = 3.162 nM | Click to Show More | [1] | |
| 2 | ENMD-2076 | Drug Info | IC50 = 10 nM | [4] | ||
| Co-Target Name | Fibroblast growth factor receptor 3 (FGFR3) | Clinical trial Target | ||||
| UniProt ID | FGFR3_HUMAN | |||||
| Gene Name | FGFR3 | |||||
| Synonyms |
JTK4; FGFR-3; CD333
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| 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
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| 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 | [6] | ||
| Co-Target Name | Protein delta homolog 1 (DLK1) | Clinical trial Target | ||||
| UniProt ID | DLK1_HUMAN | |||||
| Gene Name | DLK1 | |||||
| Synonyms |
pG2; DLK-1
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| Representative Drug(s) | VX-680 | Drug Info | Ki = 35.8 nM | [24] | ||
| Co-Target Name | Focal adhesion kinase 1 (FAK) | Clinical trial Target | ||||
| UniProt ID | FAK1_HUMAN | |||||
| Gene Name | PTK2 | |||||
| Synonyms |
pp125FAK; p125FAK; Protein-tyrosine kinase 2; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Focal adhesion kinase-related nonkinase; FRNK; FAK1; FADK 1; FADK
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| Representative Drug(s) | ENMD-2076 | Drug Info | IC50 = 55 nM | [3] | ||
| 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
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| Representative Drug(s) | VX-680 | Drug Info | IC50 = 208 nM | [25] | ||
| 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
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| Representative Drug(s) | CYC116 | Drug Info | Ki = 390 nM | Click to Show More | [11] | |
| 2 | PHA-739358 | Drug Info | IC50 = 462 nM | [10] | ||
| 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
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| Representative Drug(s) | VX-680 | Drug Info | IC50 = 420 nM | Click to Show More | [23] | |
| 2 | AT9283 | Drug Info | IC50 = 685 nM | [27] | ||
| 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
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| Representative Drug(s) | CYC116 | Drug Info | Ki = 480 nM | [11] | ||
| 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
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| Representative Drug(s) | CYC116 | Drug Info | Ki = 480 nM | [11] | ||
| 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
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| Representative Drug(s) | CYC116 | Drug Info | Ki = 540 nM | [11] | ||
| 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
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| 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
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| Representative Drug(s) | VX-680 | Drug Info | IC50 = 6.22 nM | [28] | ||
| 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
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| 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
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| Representative Drug(s) | VX-680 | Drug Info | IC50 = 18 nM | [29] | ||
| 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
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| 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
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| 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
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| 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
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| Representative Drug(s) | VX-680 | Drug Info | Ki = 11 nM | [30] | ||
| 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
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| Representative Drug(s) | PHA-739358 | Drug Info | IC50 = 621 nM | [10] | ||
| 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
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| Representative Drug(s) | VX-680 | Drug Info | Ki = 0.6 nM | [9] | ||
| Co-Target Name | Aurora kinase B-Inner centromere protein complex (AURKB-INCENP) | Co-Target | ||||
| UniProt ID | AURKB_HUMAN-INCE_HUMAN | |||||
| Gene Name | AURKB-INCENP | |||||
| Representative Drug(s) | MLN8237 | Drug Info | IC50 = 1.1 nM | Click to Show More | [17] | |
| 2 | MK-5108 | Drug Info | IC50 = 1.49 nM | [17] | ||
| 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
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| Representative Drug(s) | AT9283 | Drug Info | IC50 = 10 nM | [2] | ||
| 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 | [11] | ||
| 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 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. Eur J Med Chem. 2019 Dec 15;184:111710. | ||||
| REF 5 | Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. | ||||
| REF 6 | Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families. Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12. | ||||
| REF 7 | 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 8 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 9 | 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 10 | 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 11 | 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 12 | 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 13 | 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 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 | MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors. ACS Med Chem Lett. 2015 Apr 22;6(6):630-4. | ||||
| REF 16 | A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies. Eur J Med Chem. 2017 Nov 10;140:1-19. | ||||
| REF 17 | Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening. J Med Chem. 2016 Aug 11;59(15):7188-211. | ||||
| REF 18 | Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem. 2010 May 27;53(10):3973-4001. | ||||
| REF 19 | Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3523-30. | ||||
| REF 20 | SAR156497, an exquisitely selective inhibitor of aurora kinases. J Med Chem. 2015 Jan 8;58(1):362-75. | ||||
| REF 21 | A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem. 2009 May 28;52(10):3300-7. | ||||
| REF 22 | 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 23 | The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315. | ||||
| REF 24 | Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-87. | ||||
| REF 25 | Tozasertib Analogues as Inhibitors of Necroptotic Cell Death. J Med Chem. 2018 Mar 8;61(5):1895-920. | ||||
| REF 26 | 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4709-11. | ||||
| REF 27 | Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. Bioorg Med Chem. 2017 May 1;25(9):2609-16. | ||||
| REF 28 | Interrupting cyclic dinucleotide-cGAS-STING axis with small molecules. Med. Chem. Commun. 2019;10:1999-2023. | ||||
| REF 29 | Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62. | ||||
| REF 30 | The Discovery of Polo-Like Kinase 4 Inhibitors: Design and Optimization of Spiro[cyclopropane-1,3'[3H]indol]-2'(1'H)-ones as Orally Bioavailable Antitumor Agents. J Med Chem. 2015 Jan 8;58(1):130-46. | ||||
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