Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
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
Target Type Successful Target
Gene Name BTK
Biochemical Class Kinase
UniProt ID
BTK_HUMAN
Co-Targets of This Target  Top
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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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