Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T25005 | Target Info | |||
| Target Name | Tyrosine-protein kinase BTK (ATK) | ||||
| 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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| Target Type | Successful Target | ||||
| Gene Name | BTK | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Erbb4 tyrosine kinase receptor (Erbb-4) | Successful Target | ||||
| UniProt ID | ERBB4_HUMAN | |||||
| Gene Name | ERBB4 | |||||
| Synonyms |
Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 0.25 nM | Click to Show More | [1] | |
| 2 | M2951 | Drug Info | IC50 = 37.9 nM | [4] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 0.75 nM | Click to Show More | [1] | |
| 2 | CC-292 | Drug Info | IC50 = 442 nM | [7] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 1.5 nM | [2] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 2.85 nM | Click to Show More | [1] | |
| 2 | BMS-986142 | Drug Info | IC50 = 71 nM | [6] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 5.2 nM | [2] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 10 nM | Click to Show More | [1] | |
| 2 | CC-292 | Drug Info | IC50 = 22.5 nM | [3] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 38 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
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 ~ 1000 nM | [2] | ||
| 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) | Ibrutinib | Drug Info | IC50 ~ 1000 nM | [2] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 3 nM | Click to Show More | [1] | |
| 2 | BMS-986142 | Drug Info | IC50 = 15 nM | [6] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 18 nM | [1] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 200 nM | [8] | ||
| 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) | Ibrutinib | Drug Info | IC50 ~ 1000 nM | [2] | ||
| 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) | Ibrutinib | Drug Info | IC50 ~ 1000 nM | [2] | ||
| Co-Target Name | B lymphocyte kinase (BLK) | Patented-recorded Target | ||||
| UniProt ID | BLK_HUMAN | |||||
| Gene Name | BLK | |||||
| Synonyms |
p55-Blk; Tyrosine-protein kinase Blk
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 0.23 nM | Click to Show More | [1] | |
| 2 | BMS-986142 | Drug Info | IC50 = 23 nM | [6] | ||
| Co-Target Name | Tyrosine-protein kinase BMX (BMX) | Patented-recorded Target | ||||
| UniProt ID | BMX_HUMAN | |||||
| Gene Name | BMX | |||||
| Synonyms |
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 0.5 nM | Click to Show More | [1] | |
| 2 | BMS-986142 | Drug Info | IC50 = 32 nM | [6] | ||
| 3 | M2951 | Drug Info | IC50 = 37.9 nM | [4] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 0.5 nM | Click to Show More | [2] | |
| 2 | CC-292 | Drug Info | IC50 = 6.2 nM | [9] | ||
| 3 | BMS-986142 | Drug Info | IC50 = 10 nM | [6] | ||
| 4 | M2951 | Drug Info | IC50 = 37.9 nM | [4] | ||
| Co-Target Name | Tyrosine-protein kinase Fgr (FGR) | Literature-reported Target | ||||
| UniProt ID | FGR_HUMAN | |||||
| Gene Name | FGR | |||||
| Synonyms |
p58c-Fgr; p58-Fgr; p55-Fgr; SRC2; Proto-oncogene c-Fgr; Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 1.82 nM | [1] | ||
| 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) | Ibrutinib | Drug Info | IC50 = 2.89 nM | Click to Show More | [1] | |
| 2 | BMS-986142 | Drug Info | IC50 = 28 nM | [6] | ||
| Co-Target Name | Tyrosine-protein kinase FRK (FRK) | Co-Target | ||||
| UniProt ID | FRK_HUMAN | |||||
| Gene Name | FRK | |||||
| Synonyms |
FYN-related kinase; Nuclear tyrosine protein kinase RAK; Protein-tyrosine kinase 5
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 79 nM | [1] | ||
| Co-Target Name | Peroxiredoxin-like 2A (PRXL2A) | Co-Target | ||||
| UniProt ID | PXL2A_HUMAN | |||||
| Gene Name | PRXL2A | |||||
| Synonyms |
Peroxiredoxin-like 2 activated in M-CSF stimulated monocytes; Protein PAMM; Redox-regulatory protein FAM213A
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| Representative Drug(s) | Ibrutinib | Drug Info | IC50 = 900 nM | [10] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase. J Med Chem. 2019 Sep 12;62(17):7923-7940. | ||||
| REF 2 | Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors. J Med Chem. 2018 May 24;61(10):4608-27. | ||||
| REF 3 | Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. Eur J Med Chem. 2018 Jan 1;143:1847-57. | ||||
| REF 4 | Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem. 2018 Mar 22;61(6):2227-45. | ||||
| REF 5 | Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning. ACS Med Chem Lett. 2018 Dec 3;10(1):80-85. | ||||
| REF 6 | Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers. J Med Chem. 2016 Oct 13;59(19):9173-200. | ||||
| REF 7 | Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor. Eur J Med Chem. 2017 May 5;131:107-25. | ||||
| REF 8 | Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6258-63. | ||||
| REF 9 | The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review. Eur J Med Chem. 2018 May 10;151:315-26. | ||||
| REF 10 | Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40. | ||||
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