Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T38284 | Target Info | |||
| Target Name | Fusion protein Bcr-Abl (Bcr-Abl) | ||||
| Synonyms |
BCR-ABL fusion protein; BCR-ABL
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| Target Type | Successful Target | ||||
| Gene Name | BCR-ABL1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Drug Info | IC50 = 0.17 nM | Click to Show More | [1] | ||
| 2 | Nilotinib | Drug Info | IC50 < 2.54 nM | [8] | ||
| 3 | Drug Info | Ki = 13 nM | [11] | |||
| 4 | Bafetinib | Drug Info | IC50 = 26 nM | [14] | ||
| 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) | Drug Info | IC50 = 0.2 nM | [2] | |||
| 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) | Drug Info | Ki = 0.295 nM | [3] | |||
| 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) | Drug Info | IC50 = 0.4 nM | Click to Show More | [4] | ||
| 2 | Nilotinib | Drug Info | IC50 = 108.2 nM | [8] | ||
| 3 | Drug Info | IC50 = 160 nM | [21] | |||
| Co-Target Name | Tyrosine-protein kinase BTK (ATK) | Successful Target | ||||
| UniProt ID | BTK_HUMAN | |||||
| Gene Name | BTK | |||||
| Synonyms |
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
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| Representative Drug(s) | Drug Info | IC50 = 1.3 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
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| Representative Drug(s) | Drug Info | IC50 = 1.5 nM | Click to Show More | [6] | ||
| 2 | Nilotinib | Drug Info | IC50 < 10 nM | [8] | ||
| 3 | Drug Info | IC50 = 16.4 nM | [12] | |||
| 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) | Drug Info | IC50 = 1.995 nM | Click to Show More | [7] | ||
| 2 | Nilotinib | Drug Info | IC50 < 2.54 nM | [8] | ||
| 3 | Drug Info | IC50 = 9.9 nM | [10] | |||
| Co-Target Name | Carbonic anhydrase II (CA-II) | Successful Target | ||||
| UniProt ID | CAH2_HUMAN | |||||
| Gene Name | CA2 | |||||
| Synonyms |
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 4.1 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 30.2 nM | [9] | |||
| 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) | Drug Info | Ki < 10 nM | Click to Show More | [3] | ||
| 2 | Nilotinib | Drug Info | IC50 = 60.11 nM | [8] | ||
| 3 | Drug Info | IC50 = 72 nM | [18] | |||
| Co-Target Name | Epidermal growth factor receptor (EGFR) | Successful Target | ||||
| UniProt ID | EGFR_HUMAN | |||||
| Gene Name | EGFR | |||||
| Synonyms |
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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| Representative Drug(s) | Drug Info | IC50 = 20 nM | [13] | |||
| Co-Target Name | Carbonic anhydrase I (CA-I) | Successful Target | ||||
| UniProt ID | CAH1_HUMAN | |||||
| Gene Name | CA1 | |||||
| Synonyms |
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 29.3 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 31.9 nM | [9] | |||
| Co-Target Name | Quinone reductase 2 (NQO2) | Successful Target | ||||
| UniProt ID | NQO2_HUMAN | |||||
| Gene Name | NQO2 | |||||
| Synonyms |
Quinone oxidoreductase 2; Qui reductase 2; QR2; NRH:quinone oxidoreductase 2; NRH:qui oxidoreductase 2; NQO2; NAD(P)H qui oxidoreductase 2
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| Representative Drug(s) | Drug Info | Ki = 39 nM | Click to Show More | [15] | ||
| 2 | Nilotinib | Drug Info | IC50 = 381 nM | [22] | ||
| Co-Target Name | Solute carrier family 47 member 1 (SLC47A1) | Successful Target | ||||
| UniProt ID | S47A1_HUMAN | |||||
| Gene Name | SLC47A1 | |||||
| Synonyms |
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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| Representative Drug(s) | Drug Info | IC50 = 40 nM | [16] | |||
| Co-Target Name | Platelet-derived growth factor receptor (PDGFR) | Successful Target | ||||
| UniProt ID | PGFRA_HUMAN; PGFRB_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R
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| Representative Drug(s) | Drug Info | IC50 = 50 nM | [17] | |||
| 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) | Nilotinib | Drug Info | IC50 = 125.89 nM | [19] | ||
| 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) | Drug Info | IC50 = 131 nM | [20] | |||
| Co-Target Name | Carbonic anhydrase XIV (CA-XIV) | Successful Target | ||||
| UniProt ID | CAH14_HUMAN | |||||
| Gene Name | CA14 | |||||
| Synonyms |
UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 223 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 468 nM | [9] | |||
| Co-Target Name | Carbonic anhydrase XII (CA-XII) | Successful Target | ||||
| UniProt ID | CAH12_HUMAN | |||||
| Gene Name | CA12 | |||||
| Synonyms |
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 302 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 980 nM | [9] | |||
| Co-Target Name | Carbonic anhydrase VI (CA-VI) | Successful Target | ||||
| UniProt ID | CAH6_HUMAN | |||||
| Gene Name | CA6 | |||||
| Synonyms |
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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| Representative Drug(s) | Drug Info | Ki = 392 nM | Click to Show More | [9] | ||
| 2 | Nilotinib | Drug Info | Ki = 461 nM | [9] | ||
| 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) | Drug Info | IC50 = 433 nM | [10] | |||
| Co-Target Name | Carbonic anhydrase IV (CA-IV) | Successful Target | ||||
| UniProt ID | CAH4_HUMAN | |||||
| Gene Name | CA4 | |||||
| Synonyms |
Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 446 nM | [9] | ||
| Co-Target Name | Erbb2 tyrosine kinase receptor (HER2) | Successful Target | ||||
| UniProt ID | ERBB2_HUMAN | |||||
| Gene Name | ERBB2 | |||||
| Synonyms |
p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
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| Representative Drug(s) | Drug Info | IC50 = 710 nM | [2] | |||
| 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) | Drug Info | IC50 = 880 nM | [4] | |||
| 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) | Drug Info | IC50 < 0.5 nM | [10] | |||
| Co-Target Name | Ephrin type-B receptor 4 (EPHB4) | Clinical trial Target | ||||
| UniProt ID | EPHB4_HUMAN | |||||
| Gene Name | EPHB4 | |||||
| Synonyms |
Tyrosine-protein kinase TYRO11; TYRO11; MYK1; Hepatoma transmembrane kinase; HTK
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| Representative Drug(s) | Drug Info | IC50 < 1 nM | [13] | |||
| Co-Target Name | Tyrosine-protein kinase Lyn (JTK8) | Clinical trial Target | ||||
| UniProt ID | LYN_HUMAN | |||||
| Gene Name | LYN | |||||
| Synonyms |
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
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| Representative Drug(s) | Drug Info | IC50 = 1.2 nM | Click to Show More | [23] | ||
| 2 | Bafetinib | Drug Info | IC50 = 11 nM | [14] | ||
| 3 | Drug Info | IC50 = 220 nM | [14] | |||
| Co-Target Name | Ephrin type-B receptor 2 (EPHB2) | Clinical trial Target | ||||
| UniProt ID | EPHB2_HUMAN | |||||
| Gene Name | EPHB2 | |||||
| Synonyms |
hEK5; Tyrosine-protein kinase receptor EPH-3; Tyrosine-protein kinase TYRO5; TYRO5; Renal carcinoma antigen NY-REN-47; Receptor protein-tyrosine kinase HEK5; EphB2 receptor tyrosine kinase; EphB2; EPTH3; EPHT3; EPH-like kinase 5; EPH tyrosine kinase 3; ELK-related tyrosine kinase; EK5; Developmentally-regulated Eph-related tyrosine kinase; DRT
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| Representative Drug(s) | Drug Info | IC50 = 4.4 nM | [6] | |||
| 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) | Drug Info | IC50 = 5.012 nM | Click to Show More | [7] | ||
| 2 | Drug Info | IC50 = 291 nM | [18] | |||
| 3 | Nilotinib | Drug Info | IC50 = 677 nM | [18] | ||
| Co-Target Name | Tyrosine-protein kinase BRK (PTK6) | Clinical trial Target | ||||
| UniProt ID | PTK6_HUMAN | |||||
| Gene Name | PTK6 | |||||
| Synonyms |
Protein-tyrosine kinase 6; Breast tumor kinase; BRK
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| Representative Drug(s) | Drug Info | IC50 = 5.3 nM | [23] | |||
| Co-Target Name | Carbonic anhydrase IX (CA-IX) | Clinical trial Target | ||||
| UniProt ID | CAH9_HUMAN | |||||
| Gene Name | CA9 | |||||
| Synonyms |
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 41.9 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 75.7 nM | [9] | |||
| Co-Target Name | Stress-activated protein kinase (p38) | Clinical trial Target | ||||
| UniProt ID | MK11_HUMAN; MK12_HUMAN; MK13_HUMAN; MK14_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Synonyms |
p38) Stress-activated protein kinase; P38 MAPK; P38 MAP kinase; Mitogen-activated protein kinase p38
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| Representative Drug(s) | Drug Info | IC50 = 100 nM | [4] | |||
| Co-Target Name | Ephrin type-A receptor 2 (EPHA2) | Clinical trial Target | ||||
| UniProt ID | EPHA2_HUMAN | |||||
| Gene Name | EPHA2 | |||||
| Synonyms |
Tyrosine-protein kinase receptor ECK; Epithelial cell kinase; EphA2receptor; ECK
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| Representative Drug(s) | Drug Info | IC50 = 137 nM | [24] | |||
| Co-Target Name | Proto-oncogene c-RAF (c-RAF) | Clinical trial Target | ||||
| UniProt ID | RAF1_HUMAN | |||||
| Gene Name | RAF1 | |||||
| Synonyms |
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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| Representative Drug(s) | Drug Info | IC50 = 164 nM | [6] | |||
| Co-Target Name | T-cell-specific kinase (ITK) | Clinical trial Target | ||||
| UniProt ID | ITK_HUMAN | |||||
| Gene Name | ITK | |||||
| Synonyms |
Tyrosine kinase ITK; Inducible T cell kinase; EMT
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| Representative Drug(s) | Drug Info | IC50 = 228 nM | [5] | |||
| Co-Target Name | Stress-activated protein kinase 2a (p38 alpha) | Clinical trial Target | ||||
| UniProt ID | MK14_HUMAN | |||||
| Gene Name | MAPK14 | |||||
| Synonyms |
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
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| Representative Drug(s) | Drug Info | EC50 = 470 nM | [25] | |||
| 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) | Drug Info | IC50 = 0.4 nM | Click to Show More | [26] | ||
| 2 | Nilotinib | Drug Info | IC50 = 2 nM | [26] | ||
| 3 | Drug Info | IC50 = 141 nM | [18] | |||
| Co-Target Name | Epithelial discoidin domain receptor 1 (DDR1) | Patented-recorded Target | ||||
| UniProt ID | DDR1_HUMAN | |||||
| Gene Name | DDR1 | |||||
| Synonyms |
Tyrosine-protein kinase CAK; Tyrosine kinase DDR; TRKE; TRK E; RTK6; Protein-tyrosine kinase RTK-6; Protein-tyrosine kinase 3A; PTK3A; NTRK4; NEP; Mammary carcinoma kinase 10; MCK-10; HGK2; Epithelial discoidin domain-containing receptor 1; EDDR1; Discoidin receptor tyrosine kinase; Cell adhesion kinase; CD167a; CD167 antigen-like family member A
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| Representative Drug(s) | Drug Info | IC50 = 0.5 nM | Click to Show More | [27] | ||
| 2 | Nilotinib | Drug Info | IC50 = 3.7 nM | [18] | ||
| 3 | Drug Info | IC50 = 43 nM | [18] | |||
| Co-Target Name | Casein kinase I alpha (CSNK1A1) | Patented-recorded Target | ||||
| UniProt ID | KC1A_HUMAN | |||||
| Gene Name | CSNK1A1 | |||||
| Synonyms |
Casein kinase I isoform alpha; CKI-alpha; CK1
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| Representative Drug(s) | Drug Info | IC50 < 1 nM | [13] | |||
| Co-Target Name | Hematopoietic cell kinase (HCK) | Patented-recorded Target | ||||
| UniProt ID | HCK_HUMAN | |||||
| Gene Name | HCK | |||||
| Synonyms |
p61Hck; p59Hck; p59-HCK/p60-HCK; Tyrosine-protein kinase HCK; Hemopoietic cell kinase
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| Representative Drug(s) | Drug Info | IC50 < 1 nM | [13] | |||
| Co-Target Name | Tyrosine-protein kinase CSK (CSK) | Patented-recorded Target | ||||
| UniProt ID | CSK_HUMAN | |||||
| Gene Name | CSK | |||||
| Synonyms |
Protein-tyrosine kinase CYL; C-Src kinase
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| Representative Drug(s) | Drug Info | IC50 = 1.3 nM | [23] | |||
| Co-Target Name | Activated CDC42 kinase 1 (ACK-1) | Patented-recorded Target | ||||
| UniProt ID | ACK1_HUMAN | |||||
| Gene Name | TNK2 | |||||
| Synonyms |
Tyrosine kinase non-receptor protein 2; ACK1; ACK-1
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| Representative Drug(s) | Drug Info | Ki < 10 nM | [3] | |||
| Co-Target Name | Carbonic anhydrase VII (CA-VII) | Patented-recorded Target | ||||
| UniProt ID | CAH7_HUMAN | |||||
| Gene Name | CA7 | |||||
| Synonyms |
Carbonic anhydrase 7; Carbonate dehydratase VII
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 99 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 109 nM | [9] | |||
| Co-Target Name | Tyrosine-protein kinase Tec (PSCTK4) | Patented-recorded Target | ||||
| UniProt ID | TEC_HUMAN | |||||
| Gene Name | TEC | |||||
| Synonyms |
Tec protein tyrosine kinase
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| Representative Drug(s) | Drug Info | IC50 = 297 nM | [5] | |||
| Co-Target Name | Tyrosine-protein kinase TXK (TXK) | Literature-reported Target | ||||
| UniProt ID | TXK_HUMAN | |||||
| Gene Name | TXK | |||||
| Synonyms |
Resting lymphocyte kinase; RLK; Protein-tyrosine kinase 4; PTK4
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| Representative Drug(s) | Drug Info | IC50 = 0.3 nM | [6] | |||
| Co-Target Name | Membrane-associated kinase (PKMYT1) | Literature-reported Target | ||||
| UniProt ID | PMYT1_HUMAN | |||||
| Gene Name | PKMYT1 | |||||
| Synonyms |
Myt1 kinase; Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase; MYT1
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| Representative Drug(s) | Drug Info | Ki = 0.5 nM | [28] | |||
| 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
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| Representative Drug(s) | Drug Info | Ki < 10 nM | [3] | |||
| Co-Target Name | LIM domain kinase-1 (LIMK-1) | Literature-reported Target | ||||
| UniProt ID | LIMK1_HUMAN | |||||
| Gene Name | LIMK1 | |||||
| Synonyms |
LIMK-1; LIMK
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| Representative Drug(s) | Drug Info | IC50 = 114 nM | [6] | |||
| Co-Target Name | Tyrosine-protein kinase ABL2 (ABL2) | Literature-reported Target | ||||
| UniProt ID | ABL2_HUMAN | |||||
| Gene Name | ABL2 | |||||
| Synonyms |
Tyrosine-protein kinase ARG; Abelson-related gene protein; Abelson tyrosine-protein kinase 2; Abelson murine leukemia viral oncogene homolog 2; ARG; ABLL
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| Representative Drug(s) | Drug Info | IC50 = 272 nM | [15] | |||
| Co-Target Name | Multidrug and toxin extrusion protein 2 (MATE2) | Literature-reported Target | ||||
| UniProt ID | S47A2_HUMAN | |||||
| Gene Name | SLC47A2 | |||||
| Synonyms |
hMATE-2; Solute carrier family 47 member 2; MATE2; MATE-2; Kidney-specific H(+)/organic cation antiporter
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| Representative Drug(s) | Drug Info | IC50 = 350 nM | [16] | |||
| Co-Target Name | Serine/threonine-protein kinase RIPK2 (RIPK2) | Co-Target | ||||
| UniProt ID | RIPK2_HUMAN | |||||
| Gene Name | RIPK2 | |||||
| Synonyms |
Receptor-interacting serine/threonine-protein kinase 2; CARD-containing interleukin-1 beta-converting enzyme-associated kinase; CARD-containing IL-1 beta ICE-kinase; RIP-like-interacting CLARP kinase; Receptor-interacting protein 2; RIP-2; Tyrosine-protein kinase RIPK2
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| Representative Drug(s) | Drug Info | Ki < 10 nM | [3] | |||
| Co-Target Name | Myelin transcription factor 1 (MYT1) | Co-Target | ||||
| UniProt ID | MYT1_HUMAN | |||||
| Gene Name | MYT1 | |||||
| Synonyms |
MyT1; Myelin transcription factor I; MyTI; PLPB1; Proteolipid protein-binding protein
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| Representative Drug(s) | Drug Info | IC50 = 63 nM | [29] | |||
| Co-Target Name | Carbonic anhydrase III (CA3) | Co-Target | ||||
| UniProt ID | CAH3_HUMAN | |||||
| Gene Name | CA3 | |||||
| Synonyms |
Carbonic anhydrase 3; Carbonate dehydratase III; CA-III
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| Representative Drug(s) | Nilotinib | Drug Info | Ki = 443 nM | Click to Show More | [9] | |
| 2 | Drug Info | Ki = 528 nM | [9] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem. 2013 Feb 14;56(3):879-94. | ||||
| REF 2 | 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32. | ||||
| REF 3 | Controlling cellular distribution of drugs with permeability modifying moieties. Med. Chem. Commun. 2019;10:974-984. | ||||
| REF 4 | Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61. | ||||
| REF 5 | The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13283-8. | ||||
| REF 6 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. | ||||
| REF 7 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 8 | Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors. Bioorg Med Chem Lett. 2013 Feb 1;23(3):682-6. | ||||
| REF 9 | The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4102-6. | ||||
| REF 10 | Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710. | ||||
| REF 11 | Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. Eur J Med Chem. 2008 Dec;43(12):2665-76. | ||||
| REF 12 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15. | ||||
| REF 13 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
| REF 14 | Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. Bioorg Med Chem Lett. 2007 May 15;17(10):2712-7. | ||||
| REF 15 | Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40. | ||||
| REF 16 | Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795. | ||||
| REF 17 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | ||||
| REF 18 | Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. Bioorg Med Chem. 2010 Oct 1;18(19):6977-86. | ||||
| REF 19 | Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54. | ||||
| REF 20 | Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. J Med Chem. 2019 Dec 26;62(24):11135-11150. | ||||
| REF 21 | 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. J Med Chem. 2009 Aug 13;52(15):4743-56. | ||||
| REF 22 | Affinity-Based Selectivity Profiling of an In-Class Selective Competitive Inhibitor of Acyl Protein Thioesterase 2. ACS Med Chem Lett. 2016 Dec 9;8(2):215-20. | ||||
| REF 23 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. Eur J Med Chem. 2019 Feb 1;163:610-625. | ||||
| REF 24 | c-Src protein kinase inhibitors block assembly and maturation of dengue virus. Proc Natl Acad Sci U S A. 2007 Feb 27;104(9):3520-5. | ||||
| REF 25 | Discovery of a potent p38alpha/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies. Eur J Med Chem. 2019 Dec 1;183:111684. | ||||
| REF 26 | Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62. | ||||
| REF 27 | Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. J Med Chem. 2015 Apr 23;58(8):3287-301. | ||||
| REF 28 | Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II. Bioorg Med Chem. 2018 Aug 7;26(14):4014-4024. | ||||
| REF 29 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. Eur J Med Chem. 2013 Mar;61:41-8. | ||||
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