Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T99455 | Target Info | |||
| Target Name | HUMAN fusion protein Bcr-Abl (Bcr-Abl) | ||||
| Synonyms |
BCR-ABL fusion protein; BCR-ABL
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| Gene Name | BCR-ABL1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| 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) | Imatinib | Drug Info | IC50 = 1.995 nM | [1] | ||
| 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) | Imatinib | Drug Info | Ki = 13 nM | [2] | ||
| 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) | Imatinib | Drug Info | IC50 = 16.4 nM | [3] | ||
| 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) | Imatinib | Drug Info | Ki = 30.2 nM | [4] | ||
| 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) | Imatinib | Drug Info | Ki = 31.9 nM | [4] | ||
| 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) | Imatinib | Drug Info | Ki = 39 nM | [5] | ||
| 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) | Imatinib | Drug Info | IC50 = 40 nM | [6] | ||
| 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) | Imatinib | Drug Info | IC50 = 50 nM | [7] | ||
| 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) | Imatinib | Drug Info | IC50 = 72 nM | [8] | ||
| 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) | Imatinib | Drug Info | IC50 = 131 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
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| Representative Drug(s) | Imatinib | Drug Info | IC50 = 160 nM | [10] | ||
| 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) | Imatinib | Drug Info | Ki = 392 nM | [4] | ||
| 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) | Imatinib | Drug Info | Ki = 468 nM | [4] | ||
| 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) | Imatinib | Drug Info | Ki = 980 nM | [4] | ||
| 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) | Imatinib | Drug Info | Ki = 75.7 nM | [4] | ||
| 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) | Imatinib | Drug Info | IC50 = 220 nM | [11] | ||
| 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) | Imatinib | Drug Info | IC50 = 291 nM | [8] | ||
| 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) | Imatinib | Drug Info | IC50 = 43 nM | [8] | ||
| 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) | Imatinib | Drug Info | Ki = 109 nM | [4] | ||
| 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) | Imatinib | Drug Info | IC50 = 141 nM | [8] | ||
| 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) | Imatinib | Drug Info | IC50 = 272 nM | [5] | ||
| 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) | Imatinib | Drug Info | IC50 = 350 nM | [6] | ||
| 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) | Imatinib | Drug Info | Ki = 528 nM | [4] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002. | ||||
| REF 2 | 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 3 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15. | ||||
| REF 4 | 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 5 | Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40. | ||||
| REF 6 | 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 7 | Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43. | ||||
| REF 8 | Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. Bioorg Med Chem. 2010 Oct 1;18(19):6977-86. | ||||
| REF 9 | 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 10 | 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 11 | 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. | ||||
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