YES proto-oncogene 1, Src family tyrosine kinase | Src family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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YES proto-oncogene 1, Src family tyrosine kinase

Target id: 2284

Nomenclature: YES proto-oncogene 1, Src family tyrosine kinase

Abbreviated Name: Yes

Family: Src family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: ON :     YES proto-oncogene 1, Src family tyrosine kinase has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 543 18p11.31-p11.21 YES1 YES proto-oncogene 1, Src family tyrosine kinase
Mouse - 541 5 B1 Yes1 YES proto-oncogene 1, Src family tyrosine kinase
Rat - 489 9 q38 Yes1 YES proto-oncogene 1, Src family tyrosine kinase
Previous and Unofficial Names
c-yes | p60c-yes | p61-Yes | v-yes-1 Yamaguchi sarcoma viral oncogene homolog 1 | Yamaguchi sarcoma viral (v-yes) oncogene homolog 1 | YES proto-oncogene 1
Database Links
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Yes SH3 domain.
Resolution:  1.9Å
Species:  Human
References:  10
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
eCF506 Hs Inhibition >9.3 pIC50 6
pIC50 >9.3 (IC50 <5x10-10 M) [6]
rebastinib Hs Inhibition 8.6 – 8.8 pIC50 11
pIC50 8.6 – 8.8 (IC50 2.5x10-9 – 1.5x10-9 M) [11]
saracatinib Hs Inhibition 8.4 pIC50 8
pIC50 8.4 (IC50 4x10-9 M) [8]
ibrutinib Hs Inhibition 8.4 pIC50 2
pIC50 8.4 (IC50 4.1x10-9 M) [2]
SU6656 Hs Inhibition 7.7 pIC50 5
pIC50 7.7 (IC50 2x10-8 M) [5]
theliatinib Hs Inhibition 6.5 pIC50 12
pIC50 6.5 (IC50 3.34x10-7 M) [12]
spebrutinib Hs Inhibition 6.1 pIC50 4
pIC50 6.1 (IC50 7.23x10-7 M) [4]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
Reference: 3,13

Key to terms and symbols Click column headers to sort
Target used in screen: YES
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 9.5 pKd
PD-173955 Hs Inhibitor Inhibition 8.6 pKd
bosutinib Hs Inhibitor Inhibition 8.4 pKd
KW-2449 Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd
tamatinib Hs Inhibitor Inhibition 7.5 pKd
foretinib Hs Inhibitor Inhibition 7.3 pKd
staurosporine Hs Inhibitor Inhibition 7.3 pKd
fedratinib Hs Inhibitor Inhibition 6.9 pKd
sunitinib Hs Inhibitor Inhibition 6.9 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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.

Reference: 1,7

Key to terms and symbols Click column headers to sort
Target used in screen: Tes/YES(YES1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
Lck inhibitor Hs Inhibitor Inhibition 0.7 0.0 0.0
dasatinib Hs Inhibitor Inhibition 1.9
staurosporine Hs Inhibitor Inhibition 4.5 1.0 -0.5
SU11652 Hs Inhibitor Inhibition 5.3 2.0 -1.0
sunitinib Hs Inhibitor Inhibition 5.9
TWS119 Hs Inhibitor Inhibition 6.0 1.0 -1.0
dovitinib Hs Inhibitor Inhibition 6.3
aminopurvalanol A Hs Inhibitor Inhibition 7.0 5.0 0.0
bosutinib Hs Inhibitor Inhibition 7.3
Src kinase inhibitor I Hs Inhibitor Inhibition 8.0 9.0 4.0
Displaying the top 10 most potent ligands  View all ligands in screen »


Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. 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]

3. 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]

4. Evans E, Tester R, Aslanian S, Mazdiyasn H, Ponader S, Tesar B, Chaturvedi P, Nacht M, Stiede K, Witowski S et al.. Clinical Development of AVL - 292: A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies. Accessed on 29/10/2014. Modified on 29/10/2014.,

5. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc. Natl. Acad. Sci. U.S.A., 104 (51): 20523-8. [PMID:18077363]

6. 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]

7. 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]

8. 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]

9. Lowell CA. (2004) Src-family kinases: rheostats of immune cell signaling. Mol. Immunol., 41 (6-7): 631-43. [PMID:15220000]

10. Martín-García JM, Luque I, Mateo PL, Ruiz-Sanz J, Cámara-Artigas A. (2007) Crystallographic structure of the SH3 domain of the human c-Yes tyrosine kinase: loop flexibility and amyloid aggregation. FEBS Lett., 581 (9): 1701-6. [PMID:17418139]

11. Patel PR, Sun H, Li SQ, Shen M, Khan J, Thomas CJ, Davis MI. (2013) Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg. Med. Chem. Lett., 23 (15): 4398-403. [PMID:23787099]

12. Ren Y, Zheng J, Fan S, Wang L, Cheng M, Shi D, Zhang W, Tang R, Yu Y, Jiao L et al.. (2017) Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification. Oncotarget, 8 (31): 50832-50844. [PMID:28881608]

13. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Src family: YES proto-oncogene 1, Src family tyrosine kinase. Last modified on 26/04/2018. Accessed on 16/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY,