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SRC proto-oncogene, non-receptor tyrosine kinase

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 2206

Nomenclature: SRC proto-oncogene, non-receptor tyrosine kinase

Abbreviated Name: Src

Family: Src family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 536 20q11.23 SRC SRC proto-oncogene, non-receptor tyrosine kinase
Mouse - 541 2 78.35 cM Src Rous sarcoma oncogene
Rat - 536 3q42 Src SRC proto-oncogene, non-receptor tyrosine kinase
Previous and Unofficial Names Click here for help
ASV | c-Src | p60-Src | SRC1 | SRC proto-oncogene
Database Links Click here for help
Alphafold P12931 (Hs), P05480 (Mm), Q9WUD9 (Rn)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10
ChEMBL Target CHEMBL267 (Hs), CHEMBL3074 (Mm), CHEMBL3014 (Rn)
DrugBank Target P12931 (Hs)
Ensembl Gene ENSG00000197122 (Hs), ENSMUSG00000027646 (Mm), ENSRNOG00000009495 (Rn)
Entrez Gene 6714 (Hs), 20779 (Mm), 83805 (Rn)
Human Protein Atlas ENSG00000197122 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:6714 (Hs), mmu:20779 (Mm), rno:83805 (Rn)
OMIM 190090 (Hs)
Pharos P12931 (Hs)
RefSeq Nucleotide NM_005417 (Hs), NM_001025395 (Mm), NM_031977 (Rn)
RefSeq Protein NP_005408 (Hs), NP_001020566 (Mm), NP_114183 (Rn)
SynPHARM 81398 (in complex with bosutinib)
80251 (in complex with saracatinib)
UniProtKB P12931 (Hs), P05480 (Mm), Q9WUD9 (Rn)
Wikipedia SRC (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Three-dimensional crystal structure of the tyrosine kinase c-Src.
PDB Id:  1FMK
Resolution:  1.5Å
Species:  Human
References:  32
Image of receptor 3D structure from RCSB PDB
Description:  Structure of unphosphorylated c-Src in complex with an inhibitor (imatinib)
PDB Id:  1Y57
Ligand:  imatinib
Resolution:  1.91Å
Species:  Human
References:  9
Enzyme Reaction Click here for help
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PD166285 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pKi 24
⤷ pKi 8.1 (Ki 8.4x10-9 M) [24]
GSK-3 inhibitor XIII Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pKi 5
⤷ pKi 7.1 (Ki 8.1x10-8 M) [5]
SI306 Small molecule or natural product Hs Inhibition 6.9 pKi 15
⤷ pKi 6.9 (Ki 1.3x10-7 M) [15]
acalabrutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition <6.0 pEC50 4
⤷ pEC50 <6.0 (EC50 >1x10-6 M) [4]
elzovantinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.9 pIC50 10
⤷ pIC50 9.9 (IC50 1.4x10-10 M) [10]
eCF506 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >9.3 pIC50 12
⤷ pIC50 >9.3 (IC50 <5x10-10 M) [12]
dasatinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 23
⤷ pIC50 9.1 (IC50 8x10-10 M) [23]
bosutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 3
⤷ pIC50 9.0 (IC50 1x10-9 M) [3]
compound 2 [PMID: 15546730] Small molecule or natural product Click here for species-specific activity table Hs Inhibition >9.0 pIC50 8
⤷ pIC50 >9.0 (IC50 <1x10-9 M) [8]
dorsomorphin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 21
⤷ pIC50 8.7 (IC50 2x10-9 M) [21]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
saracatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 16
⤷ pIC50 8.6 (IC50 2.7x10-9 M) [16]
WH-4-023 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.2 pIC50 22
⤷ pIC50 8.2 (IC50 6x10-9 M) [22]
nefextinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 33
⤷ pIC50 8.2 (IC50 6x10-9 M) [33]
CCT241161 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 14
⤷ pIC50 8.0 (IC50 1x10-8 M) [14]
PP121 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 2
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [2]
ibrutinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.7 pIC50 7
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [7]
ENMD-2076 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 25
⤷ pIC50 7.7 (IC50 2x10-8 M) [25]
CCT196969 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 14
⤷ pIC50 7.5 (IC50 3x10-8 M) [14]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 18
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [18]
SU6656 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 19
⤷ pIC50 7.1 (IC50 7.3x10-8 M) [19]
NG-25 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 29
⤷ pIC50 6.9 (IC50 1.13x10-7 M) [29]
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 26
⤷ pIC50 6.6 (IC50 2.4x10-7 M) [26]
balamapimod Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.6 pIC50 6
⤷ pIC50 6.6 (IC50 2.81x10-7 M) [6]
Description: Measuring inhibition substrate phosphorylation by p60c-src tyrosine kinase in an ELISA, using an anti-phosphotyrosine detection antibody.
compound 36 [PMID: 21958547] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.5 pIC50 17
⤷ pIC50 6.5 (IC50 2.98x10-7 M) [17]
TAK-020 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.2 pIC50 27
⤷ pIC50 6.2 (IC50 6.31x10-7 M) [27]
compound 25 [PMID: 31260299] Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 34
⤷ pIC50 6.0 (IC50 9.025x10-7 M) [34]
Syk inhibitor III Small molecule or natural product Click here for species-specific activity table Hs Inhibition 4.6 pIC50 30
⤷ pIC50 4.6 (IC50 2.73x10-5 M) [30]
tirbanibulin Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 4.3 pIC50 28
⤷ pIC50 4.3 (IC50 4.6x10-5 M) [28]
Description: Low affinity is expected because the peptide substrate binding site is not well formed when Src is isolated.
KX2-361 Small molecule or natural product Hs Inhibition - - 28
⤷ [28]
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 11,31
Key to terms and symbols Click column headers to sort
Target used in screen: SRC
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.7 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,13
Key to terms and symbols Click column headers to sort
Target used in screen: cSrc/c-SRC
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.5 3.5 -1.0
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 2.1 6.0 -3.0
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.5
aminopurvalanol A Small molecule or natural product Hs Inhibitor Inhibition 3.7 28.0 2.0
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.8 75.0 9.0
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 7.6 2.0 3.0
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 11.0
Lck inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.4 5.0 -1.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 16.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Src family tyrosine kinases act as general modulators of immune cell signaling, playing diverse signaling functions, both inhibitory and stimulatory, in immunoreceptor and integrin signaling pathways [20]. It is suggested that these enzymes act as rheostats rather than on-off switches.
Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
References:  20
Immuno Cell Type:  Dendritic cells
Cell Ontology Term:   dendritic cell (CL:0000451)
Immuno Process Associations
Immuno Process:  Barrier integrity
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  T cell (activation)
Immuno Process:  Immune regulation
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Immuno Process:  Chemotaxis & migration
Immuno Process:  Cellular signalling

References

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2. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 4 (11): 691-9. [PMID:18849971]

3. Bantscheff M, Eberhard D, Abraham Y, Bastuck S, Boesche M, Hobson S, Mathieson T, Perrin J, Raida M, Rau C et al.. (2007) Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol, 25 (9): 1035-44. [PMID:17721511]

4. Barf TA, Jans CGJM, Man PADeA, Oubrie AA, Raaijmakers HCA, Rewinkel JBM, Sterrenburg J-G, Wijkmans JCHM. (2014) 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as btk inhibitors. Patent number: US20140155385 A1. Assignee: Barf TA, Jans CGJM, Man PADeA, Oubrie AA, Raaijmakers HCA, Rewinkel JBM, Sterrenburg J-G, Wijkmans JCHM. Priority date: 19/07/2011. Publication date: 05/06/2014.

5. Bebbington D, Binch H, Charrier JD, Everitt S, Fraysse D, Golec J, Kay D, Knegtel R, Mak C, Mazzei F et al.. (2009) The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett, 19 (13): 3586-92. [PMID:19447622]

6. Berger DM, Powell DW, Wu B. (2009) 3-quinolinecarbonitrile protein kinase inhibitors. Patent number: US20090062281A1. Assignee: Wyeth LLC. Priority date: 20/02/2004. Publication date: 05/03/2009.

7. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med, 374 (4): 323-32. [PMID:26641137]

8. Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S et al.. (2004) Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett, 14 (24): 6061-6. [PMID:15546730]

9. Cowan-Jacob SW, Fendrich G, Manley PW, Jahnke W, Fabbro D, Liebetanz J, Meyer T. (2005) The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation. Structure, 13 (6): 861-71. [PMID:15939018]

10. Cui JJ, Rogers EW, Ung J, Whitten J, Zhai D, Deng W, Zhang X, Huang Z, Liu J, Zhang H. (2019) Macrocyclic compounds and uses thereof. Patent number: WO2019023417A1. Assignee: Tp Therapeutics, Inc.. Priority date: 28/07/2017. Publication date: 31/01/2019.

11. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

12. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al.. (2016) 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, 59 (10): 4697-710. [PMID:27115835]

13. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

14. Girotti MR, Lopes F, Preece N, Niculescu-Duvaz D, Zambon A, Davies L, Whittaker S, Saturno G, Viros A, Pedersen M et al.. (2015) Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma. Cancer Cell, 27 (1): 85-96. [PMID:25500121]

15. Greco C, Taresco V, Pearce AK, Vasey CE, Smith S, Rahman R, Alexander , Cavanagh RJ, Musumeci F, Schenone S. (2020) Development of Pyrazolo[3,4-d]pyrimidine Kinase Inhibitors as Potential Clinical Candidates for Glioblastoma Multiforme. ACS Med Chem Lett, [Articles ASAP]. DOI: 10.1021/acsmedchemlett.9b00530

16. Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A et al.. (2006) N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J Med Chem, 49 (22): 6465-88. [PMID:17064066]

17. Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J et al.. (2011) Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett, 21 (21): 6258-63. [PMID:21958547]

18. Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR et al.. (2012) The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett, 22 (15): 4979-85. [PMID:22765894]

19. Lin J, Shen W, Xue J, Sun J, Zhang X, Zhang C. (2012) Novel oxazolo[4,5-g]quinazolin-2(1H)-ones: dual inhibitors of EGFR and Src protein tyrosine kinases. Eur J Med Chem, 55: 39-48. [PMID:22818848]

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21. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE. (2010) The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. Bioorg Med Chem Lett, 20 (22): 6394-9. [PMID:20932747]

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26. Qi B, Yang Y, Gong G, He H, Yue X, Xu X, Hu Y, Li J, Chen T, Wan X et al.. (2019) Discovery of N1-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N3-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment. Eur J Med Chem, 163: 10-27. [PMID:30503936]

27. Sabat M, Dougan DR, Knight B, Lawson JD, Scorah N, Smith CR, Taylor ER, Vu P, Wyrick C, Wang H et al.. (2021) Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one, by Fragment-Based Drug Design. J Med Chem, 64 (17): 12893-12902. [PMID:34448571]

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29. Tan L, Nomanbhoy T, Gurbani D, Patricelli M, Hunter J, Geng J, Herhaus L, Zhang J, Pauls E, Ham Y et al.. (2015) Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2). J Med Chem, 58 (1): 183-96. [PMID:25075558]

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34. Yao X, Sun X, Jin S, Yang L, Xu H, Rao Y. (2019) Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis. J Med Chem, 62 (14): 6561-6574. [PMID:31260299]

How to cite this page

Src family: SRC proto-oncogene, non-receptor tyrosine kinase. Last modified on 06/03/2024. Accessed on 07/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2206.