Target Information
Target General Infomation | |||||
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Target ID |
T85943
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Former ID |
TTDS00247
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Target Name |
Proto-oncogene tyrosine-protein kinase SRC
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Gene Name |
SRC
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Synonyms |
C-SRC tyrosine kinase; C-Src; C-src TK; P60-Src; Pp60(src); Src tyrosine kinase; Tyrosine kinase; Tyrosine kinase (pp60(src)); SRC
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Target Type |
Successful
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Disease | Advanced breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33] | |||||
Chronic myelogenous leukaemia [ICD9: 205.1; ICD10: C92.1] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Glioblastoma multiforme [ICD9: 191; ICD10: C71] | |||||
Ischemia [ICD9: 459.89; ICD10: I99.8] | |||||
Multiple myeloma [ICD9: 203; ICD10: C90] | |||||
Osteosarcoma; Hematological malignancies; Solid tumours [ICD9: 140-199, 140-239, 170, 200-209, 210-229; ICD10: C40-C41, C81-C86, D10-D36, D3A] | |||||
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890] | |||||
Function |
Due to functional redundancy between members of the SRC kinase family, identification of the specific role of each SRC kinase is very difficult. SRC appears to be one of the primary kinases activated following engagement of receptors and plays a role in the activation of other protein tyrosine kinase (PTK) families. Receptor clustering or dimerization leads to recruitment of SRC to the receptor complexes where it phosphorylates the tyrosine residues within the receptor cytoplasmic domains. Plays an important role in the regulation of cytoskeletal organization through phosphorylation of specific substrates such as AFAP1.
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BioChemical Class |
Kinase
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Target Validation |
T85943
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UniProt ID | |||||
EC Number |
EC 2.7.10.2
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Sequence |
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAE
PKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGD WWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRES ETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGL CHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTL KPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKY LRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYT ARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVER GYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL |
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Structure |
1A07; 1A08; 1A09; 1A1A; 1A1B; 1A1C; 1A1E; 1FMK; 1HCS; 1HCT; 1KSW; 1O41; 1O42; 1O43; 1O44; 1O45; 1O46; 1O47; 1O48; 1O49; 1O4A; 1O4B; 1O4C; 1O4D; 1O4E; 1O4F; 1O4G; 1O4H; 1O4I; 1O4J; 1O4K; 1O4L; 1O4M; 1O4N; 1O4O; 1O4P; 1O4Q; 1O4R; 1SHD; 1Y57; 1YI6; 1YOJ; 1YOL; 1YOM;2BDF; 2BDJ; 2H8H; 2SRC; 3VRO; 3ZMP; 3ZMQ; 4F59; 4F5A; 4F5B; 4HXJ; 4K11; 4MXO; 4MXX; 4MXY; 4MXZ; 1A07; 1A08; 1A09; 1A1A; 1A1B; 1A1C; 1A1E; 1FMK; 1HCS; 1HCT; 1KSW; 1O41; 1O42; 1O43; 1O44; 1O45; 1O46; 1O47; 1O48; 1O49; 1O4A; 1O4B; 1O4C; 1O4D; 1O4E; 1O4F; 1O4G; 1O4H; 1O4I; 1O4J; 1O4K; 1O4L; 1O4M; 1O4N; 1O4O; 1O4P; 1O4Q; 1O4R;1SHD; 1Y57; 1YI6; 1YOJ; 1YOL; 1YOM; 2BDF; 2BDJ; 2H8H; 2SRC; 3VRO; 3ZMP; 3ZMQ; 4F59; 4F5A; 4F5B; 4HXJ; 4K11; 4MXO; 4MXX; 4MXY; 4MXZ
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Drugs and Mode of Action | |||||
Drug(s) | Bosutinib | Drug Info | Approved | Advanced breast cancer | [525021], [541049] |
Dasatinib | Drug Info | Approved | Chronic myelogenous leukaemia | [528715], [536577], [541021], [551871] | |
Herbimycin A | Drug Info | Approved | Cancer | [537902], [541254] | |
SKI-758 | Drug Info | Approved | Ischemia | [532210], [551871] | |
AZD0530 | Drug Info | Phase 2 | Osteosarcoma; Hematological malignancies; Solid tumours | [536957], [542701] | |
Dasatinib | Drug Info | Phase 2 | Multiple myeloma | [536957], [541021] | |
PD173074 | Drug Info | Phase 2 | Discovery agent | [468136], [523642] | |
KX-02 | Drug Info | Phase 1 | Brain cancer | [549581] | |
KX2-361 | Drug Info | Phase 1 | Glioblastoma multiforme | [525042] | |
AP22408 | Drug Info | Terminated | Osteoporosis | [546858] | |
PD166285 | Drug Info | Terminated | Discovery agent | [542988], [546594] | |
Inhibitor | 2-(4-CARCOXY-5-ISOPROPYLTHIAZOLYL)BENZOPIPERIDINE | Drug Info | [551374] | ||
3-(3-aminobenzo[e][1,2,4]triazin-7-yl)phenol | Drug Info | [528392] | |||
4-Chloro-5,7-diphenyl-7H-pyrrolo[2,3-d]pyrimidine | Drug Info | [525793] | |||
5,7-Diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ol | Drug Info | [525793] | |||
7-(naphthalen-2-yl)benzo[e][1,2,4]triazin-3-amine | Drug Info | [528392] | |||
A-420983 | Drug Info | [527057] | |||
A-770041 | Drug Info | [527790] | |||
Ac-Cys-Ile-cyclo[Phe-Lys]-Tyr-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Phe(4-NO2)-Lys-Phe(4-NO2)-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Phe(4-NO2) | Drug Info | [528214] | |||
Ac-Cys-Ile-Phe(4-NO2)-Lys-Tyr-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-Cl)-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-CN)-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-I)-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-N3)-Tyr | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Phe(4-NO2) | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Phe(4-NO2)-Tyr-Phe | Drug Info | [528214] | |||
Ac-Cys-Ile-Tyr-Lys-Tyr-Phe(4-NO2) | Drug Info | [528214] | |||
AG-1879 | Drug Info | [529039] | |||
AP-24163 | Drug Info | [530244] | |||
AP-24226 | Drug Info | [530244] | |||
AP22408 | Drug Info | [535031] | |||
BAS-00387275 | Drug Info | [528211] | |||
BAS-00387328 | Drug Info | [528211] | |||
BAS-00387347 | Drug Info | [528211] | |||
BAS-00672722 | Drug Info | [528211] | |||
BAS-01047341 | Drug Info | [528211] | |||
BAS-01047655 | Drug Info | [528211] | |||
BAS-01373578 | Drug Info | [528211] | |||
BAS-0338868 | Drug Info | [529217] | |||
BAS-0338872 | Drug Info | [529217] | |||
BAS-09534324 | Drug Info | [528211] | |||
BAS-450225 | Drug Info | [528211] | |||
BAS-4844343 | Drug Info | [528211] | |||
BMS-279700 | Drug Info | [528520] | |||
Bosutinib | Drug Info | [536474] | |||
CGP 77675 | Drug Info | [534864] | |||
CGP-191 | Drug Info | [525793] | |||
CGP-62464 | Drug Info | [525793] | |||
compound 2 | Drug Info | [527295] | |||
compound 8h | Drug Info | [531959] | |||
Cyclo[Ac-Cys-Ile-Phe]-Lys-Tyr-Tyr | Drug Info | [528214] | |||
Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Phe] | Drug Info | [528214] | |||
Cyclo[Ac-Cys-Ile-Tyr-Lys-Tyr-Tyr] | Drug Info | [528214] | |||
Cysteine Sulfenic Acid | Drug Info | [551391] | |||
Dasatinib | Drug Info | [536331], [536474], [536797] | |||
DPI59 | Drug Info | [551374] | |||
Glu-Pro-Gln-F2Pmp-Glu-Glu-Ile-Pro-Ile-Tyr-Leu | Drug Info | [551322] | |||
Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu | Drug Info | [551322] | |||
Herbimycin A | Drug Info | [537902] | |||
ISO24 | Drug Info | [551374] | |||
JNJ-10198409 | Drug Info | [527932] | |||
K00244 | Drug Info | [530144] | |||
KX-02 | Drug Info | [551070] | |||
KX2-361 | Drug Info | [543576] | |||
N-(4-PHENYLAMINO-QUINAZOLIN-6-YL)-ACRYLAMIDE | Drug Info | [551374] | |||
N-Phenyl-5-phenylimidazo[1,5-a]pyrazin-8-amine | Drug Info | [528520] | |||
N6-Benzyl Adenosine-5'-Diphosphate | Drug Info | [551393] | |||
NG-25 | Drug Info | [532902] | |||
NM-PP1 | Drug Info | [529039] | |||
Oxalic Acid | Drug Info | [551393] | |||
PAS219 | Drug Info | [551374] | |||
PASBN | Drug Info | [551374] | |||
PD-0166326 | Drug Info | [530497] | |||
PD-0173952 | Drug Info | [525862] | |||
PD-0173955 | Drug Info | [525862] | |||
PD-0173956 | Drug Info | [530497] | |||
PD-0173958 | Drug Info | [525862] | |||
PD-0179483 | Drug Info | [525862] | |||
PD-0180970 | Drug Info | [525862] | |||
PD-174265 | Drug Info | [530156] | |||
PD166285 | Drug Info | [534952] | |||
PD173074 | Drug Info | [534952] | |||
Phenylphosphate | Drug Info | [551391] | |||
Phosphonotyrosine | Drug Info | [551393] | |||
PP121 | Drug Info | [529744] | |||
RU78191 | Drug Info | [551374] | |||
RU78262 | Drug Info | [551374] | |||
RU78299 | Drug Info | [551374] | |||
RU78300 | Drug Info | [551374] | |||
RU78783 | Drug Info | [551393] | |||
RU79072 | Drug Info | [551374] | |||
RU79073 | Drug Info | [551374] | |||
RU79256 | Drug Info | [551374] | |||
RU81843 | Drug Info | [551393] | |||
RU82129 | Drug Info | [551393] | |||
RU82197 | Drug Info | [551391] | |||
RU82209 | Drug Info | [551393] | |||
RU83876 | Drug Info | [551393] | |||
RU84687 | Drug Info | [551374] | |||
RU85053 | Drug Info | [551393] | |||
RU85493 | Drug Info | [551393] | |||
RU90395 | Drug Info | [551393] | |||
SBB007833 | Drug Info | [528930] | |||
SKI-758 | Drug Info | [528584] | |||
SKS-927 | Drug Info | [528592] | |||
SU 6656 | Drug Info | [529039] | |||
TG-100435 | Drug Info | [528527] | |||
WH-4-023 | Drug Info | [528352] | |||
Y-c[D-Pen-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(2R,3R)-2-Me-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(2R,3S)-2-Me-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(2S,3R)-2-Me-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(2S,3S)-2-Me-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(3,5-diI)Tyr-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-(3-I)Tyr-GSFC]KR-NH2 | Drug Info | [534651] | |||
Y-c[D-Pen-D-(2')Nal-GSFC]KR-NH2 | Drug Info | [534651] | |||
Modulator | AZD0530 | Drug Info | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | ErbB signaling pathway | ||||
Rap1 signaling pathway | |||||
Chemokine signaling pathway | |||||
Endocytosis | |||||
VEGF signaling pathway | |||||
Focal adhesion | |||||
Adherens junction | |||||
Tight junction | |||||
Gap junction | |||||
Platelet activation | |||||
GABAergic synapse | |||||
Inflammatory mediator regulation of TRP channels | |||||
Regulation of actin cytoskeleton | |||||
GnRH signaling pathway | |||||
Estrogen signaling pathway | |||||
Prolactin signaling pathway | |||||
Thyroid hormone signaling pathway | |||||
Oxytocin signaling pathway | |||||
Bacterial invasion of epithelial cells | |||||
Epithelial cell signaling in Helicobacter pylori infection | |||||
Shigellosis | |||||
Tuberculosis | |||||
Hepatitis B | |||||
Viral carcinogenesis | |||||
Proteoglycans in cancer | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
PANTHER Pathway | Angiogenesis | ||||
Cadherin signaling pathway | |||||
Integrin signalling pathway | |||||
Parkinson disease | |||||
CCKR signaling map ST | |||||
Pathway Interaction Database | Endothelins | ||||
Signaling events mediated by PRL | |||||
LPA receptor mediated events | |||||
Atypical NF-kappaB pathway | |||||
Glypican 1 network | |||||
Plasma membrane estrogen receptor signaling | |||||
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) | |||||
Signaling events mediated by PTP1B | |||||
S1P3 pathway | |||||
EPHB forward signaling | |||||
Nectin adhesion pathway | |||||
Regulation of p38-alpha and p38-beta | |||||
CDC42 signaling events | |||||
Signaling events regulated by Ret tyrosine kinase | |||||
Arf6 signaling events | |||||
Signaling events mediated by TCPTP | |||||
FAS (CD95) signaling pathway | |||||
Thromboxane A2 receptor signaling | |||||
Netrin-mediated signaling events | |||||
Alpha9 beta1 integrin signaling events | |||||
CXCR4-mediated signaling events | |||||
EGF receptor (ErbB1) signaling pathway | |||||
Class I PI3K signaling events | |||||
Posttranslational regulation of adherens junction stability and dissassembly | |||||
Regulation of Androgen receptor activity | |||||
E-cadherin signaling in the nascent adherens junction | |||||
amb2 Integrin signaling | |||||
Integrins in angiogenesis | |||||
ErbB1 downstream signaling | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
ErbB2/ErbB3 signaling events | |||||
EPHA forward signaling | |||||
E-cadherin signaling in keratinocytes | |||||
PDGFR-beta signaling pathway | |||||
Nongenotropic Androgen signaling | |||||
Internalization of ErbB1 | |||||
CXCR3-mediated signaling events | |||||
Signaling events mediated by VEGFR1 and VEGFR2 | |||||
Syndecan-2-mediated signaling events | |||||
Class I PI3K signaling events mediated by Akt | |||||
Syndecan-3-mediated signaling events | |||||
Ephrin B reverse signaling | |||||
Trk receptor signaling mediated by PI3K and PLC-gamma | |||||
EPHA2 forward signaling | |||||
Alpha-synuclein signaling | |||||
FGF signaling pathway | |||||
Alpha4 beta1 integrin signaling events | |||||
Signaling events mediated by focal adhesion kinase | |||||
WikiPathways | ErbB Signaling Pathway | ||||
Senescence and Autophagy in Cancer | |||||
Notch Signaling Pathway | |||||
EPO Receptor Signaling | |||||
EGF/EGFR Signaling Pathway | |||||
TGF beta Signaling Pathway | |||||
Signaling of Hepatocyte Growth Factor Receptor | |||||
Kit receptor signaling pathway | |||||
Pregnane X Receptor pathway | |||||
Aryl Hydrocarbon Receptor Pathway | |||||
IL-3 Signaling Pathway | |||||
Nanoparticle-mediated activation of receptor signaling | |||||
Polycystic Kidney Disease Pathway | |||||
Alpha 6 Beta 4 signaling pathway | |||||
BDNF signaling pathway | |||||
Integrated Pancreatic Cancer Pathway | |||||
Oncostatin M Signaling Pathway | |||||
Interleukin-11 Signaling Pathway | |||||
AGE/RAGE pathway | |||||
Signaling Pathways in Glioblastoma | |||||
TSLP Signaling Pathway | |||||
Arylhydrocarbon receptor (AhR) signaling pathway | |||||
Regulation of Microtubule Cytoskeleton | |||||
FSH signaling pathway | |||||
Leptin signaling pathway | |||||
RANKL/RANK Signaling Pathway | |||||
Integrin-mediated Cell Adhesion | |||||
Angiogenesis | |||||
Androgen receptor signaling pathway | |||||
References | |||||
Ref 468136 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5037). | ||||
Ref 523642 | ClinicalTrials.gov (NCT01441297) BIBF 1120 as Second Line Treatment for Small Cell Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 525021 | ClinicalTrials.gov (NCT02311998) Phase I/II Study of Bosutinib in Combination With Inotuzumab Ozogamicin in CD22-positive Philadelphia-Chromosome (PC) Positive Acute Lymphoblastic Leukemia (ALL) and Chronic Myeloid Leukemia (CML). U.S. National Institutes of Health. | ||||
Ref 525042 | ClinicalTrials.gov (NCT02326441) Safety, Tolerability & PK of KX2-361 in Subjects w Adv. Malignancies Refractory to Conventional Therapies. U.S. National Institutes of Health. | ||||
Ref 536577 | Dasatinib: a tyrosine kinase inhibitor for the treatment of chronic myelogenous leukemia and philadelphia chromosome-positive acute lymphoblastic leukemia. Clin Ther. 2007 Nov;29(11):2289-308. | ||||
Ref 536957 | Current and future treatments of bone metastases. Expert Opin Emerg Drugs. 2008 Dec;13(4):609-27. | ||||
Ref 537902 | In vivo antitumor activity of herbimycin A, a tyrosine kinase inhibitor, targeted against BCR/ABL oncoprotein in mice bearing BCR/ABL-transfected cells. Leuk Res. 1994 Nov;18(11):867-73. | ||||
Ref 541021 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5678). | ||||
Ref 541049 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5710). | ||||
Ref 541254 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5984). | ||||
Ref 542701 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7731). | ||||
Ref 542988 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8183). | ||||
Ref 546594 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009107) | ||||
Ref 546858 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010691) | ||||
Ref 525793 | Bioorg Med Chem Lett. 2000 May 1;10(9):945-9.Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src. | ||||
Ref 525862 | Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. | ||||
Ref 527057 | Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. | ||||
Ref 527295 | Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6. | ||||
Ref 527790 | Bioorg Med Chem Lett. 2006 Jan 1;16(1):118-22. Epub 2005 Oct 10.Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection. | ||||
Ref 527932 | J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. | ||||
Ref 528211 | J Med Chem. 2006 Jun 1;49(11):3278-86.A combination of docking/dynamics simulations and pharmacophoric modeling to discover new dual c-Src/Abl kinase inhibitors. | ||||
Ref 528214 | J Med Chem. 2006 Jun 1;49(11):3395-401.Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors. | ||||
Ref 528352 | Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem. 2006 Aug 10;49(16):4981-91. | ||||
Ref 528392 | Bioorg Med Chem Lett. 2006 Nov 1;16(21):5546-50. Epub 2006 Aug 22.Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors. | ||||
Ref 528520 | Bioorg Med Chem. 2007 Jan 15;15(2):868-85. Epub 2006 Oct 24.Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke. | ||||
Ref 528527 | Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. | ||||
Ref 528584 | J Med Chem. 2006 Dec 28;49(26):7868-76.Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. | ||||
Ref 528592 | Bioorg Med Chem Lett. 2007 Mar 1;17(5):1358-61. Epub 2006 Dec 3.Inhibition of Src kinase activity by 7-ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of SKS-927. | ||||
Ref 528930 | Synthesis and pharmacological evaluation of novel beta-nitrostyrene derivatives as tyrosine kinase inhibitors with potent antiplatelet activity. Biochem Pharmacol. 2007 Aug 15;74(4):601-11. Epub 2007 Jun 3. | ||||
Ref 529039 | Biochem J. 2007 Dec 15;408(3):297-315.The selectivity of protein kinase inhibitors: a further update. | ||||
Ref 529217 | Bioorg Med Chem Lett. 2008 Feb 1;18(3):1207-11. Epub 2007 Dec 4.Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents. | ||||
Ref 529744 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
Ref 530144 | The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92. | ||||
Ref 530156 | J Med Chem. 2009 Jul 9;52(13):3915-26.Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. | ||||
Ref 530244 | J Med Chem. 2009 Aug 13;52(15):4743-56.9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. | ||||
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