EPH receptor A2
Kinase structure
Kinase:EPHA2 (EphA2)
Family:Eph
Group:TK
Species:HUMAN
IUPHAR/BPS ID:1822
PDB:5IA4
sc-PDB:
KIDFamMap:Search
Release date:2016-11-09
PubMed: 27685543
Chain:A
(Alternate) Model:A
Orthosteric ligand:88Z
2D structure of the orthosteric ligand
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The orthosteric binding pocket


More entries for 5IA4
5IA4Alternative model: BChain: A


Structural information
DFG conformation:out
αC-helix conformation:in
G-rich loop angle (distance):66.6° (20.8Å)
G-rich loop rotation:44°
Quality Score:8
Resolution:1.8 Å
Missing Residues:0
Missing Atoms:0
Ligand binding mode
PocketsSubpocketsWaters
front
gate
back
BP-I-A
BP-I-B
BP-II-out
BP-III
Cluster
I1
Ligand
No
Protein
Yes

Pocket alignment
Uniprot sequence:KVIGAGEFGEVYKVAIKTLDFLGEAGIMGQFSHNIIRLEGVMIITEYMENGALDKFLREYLANMNYVHRDLAARNILVVSDFGLS
Sequence structure:KVIGAGEFGEVYKVAIKTLDFLGEAGIMGQFSHNIIRLEGVMIITEYMENGALDKFLREYLANMNYVHRDLAARNILVVSDFGLS

Ligand affinity
ChEMBL ID:CHEMBL1230609
Bioaffinities: 335 records for 188 kinases
Species Kinase (ChEMBL naming) Median Min Max Type Records
Homo sapiensALK tyrosine kinase receptor7.27.27.2pKd1
Homo sapiensAMP-activated protein kinase, alpha-1 subunit6.16.16.1pKd1
Homo sapiensAMP-activated protein kinase, alpha-2 subunit5.95.95.9pKd1
Homo sapiensAnkyrin repeat and protein kinase domain-containing protein 15.85.85.8pKd1
Plasmodium falciparum (isolate 3D7)Calcium-dependent protein kinase 16.66.66.6pKd1
Homo sapiensCaM kinase I alpha5.25.25.2pKd1
Homo sapiensCaM kinase I delta5.35.35.3pKd1
Homo sapiensCaM-kinase kinase alpha6.36.36.3pKd1
Homo sapiensCaM-kinase kinase beta5.45.45.4pKd1
Homo sapiensCasein kinase I epsilon5.35.35.3pKd1
Homo sapiensCasein kinase II alpha (prime)5.65.65.6pKd1
Homo sapiensCell division cycle 2-like protein kinase 67.17.17.1pKd1
Homo sapiensCell division protein kinase 86.96.96.9pKd1
Homo sapiensCitron Rho-interacting kinase5.55.55.5pKd1
Homo sapiensc-Jun N-terminal kinase 15.25.25.2pKd1
Homo sapiensc-Jun N-terminal kinase 26.26.26.2pKd1
Homo sapiensc-Jun N-terminal kinase 35.45.45.4pKd1
Homo sapiensCyclin-dependent kinase 78.48.48.4pKd1
Homo sapiensCyclin-dependent kinase 95.85.85.8pKd1
Homo sapiensCyclin-dependent kinase-like 26.66.66.6pKd1
Homo sapiensCyclin-dependent kinase-like 35.45.45.4pKd1
Homo sapiensCyclin-dependent kinase-like 55.65.65.6pKd1
Homo sapiensDeath-associated protein kinase 35.55.55.5pKd1
Homo sapiensDiscoidin domain-containing receptor 28.48.48.4pKd1
Homo sapiensDual specificity mitogen-activated protein kinase kinase 17.97.97.9pKd1
Homo sapiensDual specificity mitogen-activated protein kinase kinase 27.97.97.9pKd1
Homo sapiensDual specificity mitogen-activated protein kinase kinase 58.68.68.6pKd1
Homo sapiensDual specificity protein kinase CLK46.16.16.1pKd1
Homo sapiensDual specificity protein kinase TTK6.46.46.4pKd1
Homo sapiensDual specificity testis-specific protein kinase 16.66.66.6pKd1
Homo sapiensDual-specificity tyrosine-phosphorylation regulated kinase 25.75.75.7pKd1
Homo sapiensDual specificty protein kinase CLK16.36.36.3pKd1
Homo sapiensEphrin type-A receptor 18.28.28.2pKd1
Homo sapiensEphrin type-A receptor 28.48.48.4pKd1
Homo sapiensEphrin type-A receptor 3999pKd1
Homo sapiensEphrin type-A receptor 48.78.78.7pKd1
Homo sapiensEphrin type-A receptor 58.28.28.2pKd1
Homo sapiensEphrin type-A receptor 6999pKd1
Homo sapiensEphrin type-A receptor 78.68.68.6pKd1
Homo sapiensEphrin type-A receptor 88.78.78.7pKd1
Homo sapiensEphrin type-B receptor 17.97.97.9pKd1
Homo sapiensEphrin type-B receptor 28.48.48.4pKd1
Homo sapiensEphrin type-B receptor 37.17.17.1pKd1
Homo sapiensEphrin type-B receptor 47.97.97.9pKd1
Homo sapiensEpidermal growth factor receptor erbB15.55.55.5pIC503
Homo sapiensEpidermal growth factor receptor erbB16.55.87.1pKd12
Homo sapiensEpithelial discoidin domain-containing receptor 19.79.79.7pKd2
Homo sapiensEukaryotic translation initiation factor 2-alpha kinase 1666pKd1
Homo sapiensFibroblast growth factor receptor 16.26.26.2pKd1
Homo sapiensFibroblast growth factor receptor 26.16.16.1pKd1
Homo sapiensFibroblast growth factor receptor 35.85.86pKd2
Homo sapiensFocal adhesion kinase 16.86.86.8pKd1
Homo sapiensHepatocyte growth factor receptor8.87.79.4pIC5043
Homo sapiensHepatocyte growth factor receptor98.99.1pKd3
Homo sapiensHomeodomain-interacting protein kinase 16.46.46.4pKd1
Homo sapiensHomeodomain-interacting protein kinase 26.76.76.7pKd1
Homo sapiensHomeodomain-interacting protein kinase 37.47.47.4pKd1
Homo sapiensHomeodomain-interacting protein kinase 49.39.39.3pKd1
Homo sapiensHormonally up-regulated neu tumor-associated kinase5.35.35.3pKd1
Homo sapiensInhibitor of nuclear factor kappa B kinase alpha subunit5.25.25.2pKd1
Homo sapiensInhibitor of nuclear factor kappa B kinase epsilon subunit5.95.95.9pKd1
Homo sapiensInsulin-like growth factor I receptor6.46.46.4pKd1
Homo sapiensInsulin receptor6.76.76.7pKd1
Homo sapiensInsulin receptor-related protein7.37.37.3pKd1
Homo sapiensInterleukin-1 receptor-associated kinase 36.46.46.4pKd1
Homo sapiensLeukocyte tyrosine kinase receptor777pKd1
Homo sapiensLIM domain kinase 16.26.26.2pKd1
Homo sapiensLIM domain kinase 25.85.85.8pKd1
Homo sapiensMacrophage colony stimulating factor receptor8.78.78.7pKd1
Homo sapiensMacrophage-stimulating protein receptor8.58.58.5pIC506
Homo sapiensMacrophage-stimulating protein receptor8.58.58.5pKd1
Homo sapiensMAP kinase-interacting serine/threonine-protein kinase MNK17.17.17.1pKd1
Homo sapiensMAP kinase p38 alpha6.56.56.5pKd1
Homo sapiensMAP kinase p38 beta6.16.16.1pKd1
Homo sapiensMAP kinase p38 delta7.37.37.3pKd1
Homo sapiensMAP kinase p38 gamma6.46.46.4pKd1
Homo sapiensMAP kinase signal-integrating kinase 28.48.48.4pKd1
Homo sapiensMaternal embryonic leucine zipper kinase6.56.56.5pKd1
Homo sapiensMisshapen-like kinase 15.65.65.6pKd1
Homo sapiensMitogen-activated protein kinase 157.17.17.1pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 106.36.36.3pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 116.56.56.5pKd2
Homo sapiensMitogen-activated protein kinase kinase kinase 127.77.77.7pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 137.87.87.8pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 25.75.75.7pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 35.35.35.3pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 45.75.75.7pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 76.36.36.3pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase 9666pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase kinase 17.47.47.4pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase kinase 25.75.75.7pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase kinase 3777pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase kinase 46.76.76.7pKd1
Homo sapiensMitogen-activated protein kinase kinase kinase kinase 58.48.48.4pKd1
Homo sapiensMixed lineage kinase 77.47.47.4pKd1
Homo sapiensMuscle, skeletal receptor tyrosine protein kinase7.97.97.9pKd1
Homo sapiensMyosin IIIA5.65.65.6pKd1
Homo sapiensMyosin-IIIB6.26.26.2pKd1
Homo sapiensMyosin light chain kinase5.55.55.5pKd1
Homo sapiensmyosin light chain kinase 25.65.65.6pKd1
Homo sapiensNerve growth factor receptor Trk-A8.38.38.3pKd1
Homo sapiensNeurotrophic tyrosine kinase receptor type 28.48.48.4pKd1
Homo sapiensNon-receptor tyrosine-protein kinase TNK17.77.77.7pKd1
Homo sapiensNT-3 growth factor receptor8.58.58.5pKd1
Homo sapiensPITSLRE serine/threonine-protein kinase CDC2L16.26.26.2pKd1
Homo sapiensPITSLRE serine/threonine-protein kinase CDC2L26.36.36.3pKd1
Homo sapiensPlatelet-derived growth factor receptor alpha8.48.28.4pIC503
Homo sapiensPlatelet-derived growth factor receptor alpha8.48.48.4pKd1
Homo sapiensPlatelet-derived growth factor receptor beta888pIC502
Homo sapiensPlatelet-derived growth factor receptor beta999pKd1
Homo sapiensProtein kinase C nu5.15.15.1pKd1
Homo sapiensProtein tyrosine kinase 2 beta7.97.97.9pKd1
Homo sapiensProto-oncogene tyrosine-protein kinase MER9.69.69.6pKd1
Homo sapiensProto-oncogene tyrosine-protein kinase ROS888pIC501
Homo sapiensProto-oncogene tyrosine-protein kinase ROS7.97.97.9pKd1
Homo sapiensProto-oncogene tyrosine-protein kinase ROS7.87.78.1pKi3
Homo sapiensReceptor-interacting serine/threonine-protein kinase 16.16.16.1pKd1
Homo sapiensReceptor-interacting serine/threonine-protein kinase 46.16.16.1pKd1
Homo sapiensReceptor protein-tyrosine kinase erbB-26.26.26.2pKd1
Homo sapiensReceptor protein-tyrosine kinase erbB-46.26.26.2pKd1
Homo sapiensReceptor tyrosine-protein kinase erbB-35.85.85.8pKd1
Homo sapiensRho-associated protein kinase 25.85.85.8pKd1
Homo sapiensRibosomal protein S6 kinase 15.95.95.9pKd1
Homo sapiensRibosomal protein S6 kinase alpha 25.35.35.3pKd2
Homo sapiensSerine/threonine-protein kinase 109.39.39.3pKd1
Homo sapiensSerine/threonine-protein kinase 28.58.58.5pKd1
Homo sapiensSerine/threonine-protein kinase 255.25.25.2pKd1
Homo sapiensSerine/threonine-protein kinase 33777pKd1
Homo sapiensSerine/threonine-protein kinase 356.66.66.6pKd1
Homo sapiensSerine/threonine-protein kinase 366.86.86.8pKd1
Homo sapiensSerine/threonine-protein kinase Aurora-A5.95.86.4pKd3
Homo sapiensSerine/threonine-protein kinase Aurora-B7.47.47.4pKd1
Homo sapiensSerine/threonine-protein kinase Aurora-C7.97.97.9pKd1
Homo sapiensSerine/threonine-protein kinase B-raf5.55.55.6pKd2
Homo sapiensSerine/threonine-protein kinase Chk27.27.27.2pKd1
Homo sapiensSerine/threonine-protein kinase MAK5.85.85.8pKd1
Homo sapiensSerine/threonine-protein kinase MRCK-A6.26.26.2pKd1
Homo sapiensSerine/threonine-protein kinase MRCK beta6.56.56.5pKd1
Homo sapiensSerine/threonine-protein kinase MRCK gamma6.86.86.8pKd1
Homo sapiensSerine/threonine-protein kinase MST1666pKd1
Homo sapiensSerine/threonine-protein kinase NEK96.36.36.3pKd1
Homo sapiensSerine/threonine protein kinase NLK6.86.86.8pKd1
Homo sapiensSerine/threonine-protein kinase PAK 35.45.45.4pKd1
Homo sapiensSerine/threonine-protein kinase PCTAIRE-16.16.16.1pKd1
Homo sapiensSerine/threonine-protein kinase PCTAIRE-26.86.86.8pKd1
Homo sapiensSerine/threonine-protein kinase PCTAIRE-36.66.66.6pKd1
Homo sapiensSerine/threonine-protein kinase PFTAIRE-17.57.57.5pKd1
Homo sapiensSerine/threonine-protein kinase PFTAIRE-27.57.57.5pKd1
Homo sapiensSerine/threonine-protein kinase PLK48.58.58.5pKd1
Homo sapiensSerine/threonine-protein kinase RAF5.45.45.4pKd1
Homo sapiensSerine/threonine-protein kinase RIPK27.77.77.7pKd1
Homo sapiensSerine/threonine-protein kinase SIK16.86.86.8pKd1
Homo sapiensSerine/threonine-protein kinase SIK26.26.26.2pKd1
Homo sapiensSerine/threonine-protein kinase TAO15.45.45.4pKd1
Homo sapiensSerine/threonine-protein kinase TAO25.25.25.2pKd1
Homo sapiensSerine/threonine-protein kinase TBK16.16.16.1pKd1
Homo sapiensSerine/threonine-protein kinase TNNI3K6.96.96.9pKd1
Homo sapiensSerine/threonine-protein kinase ULK36.46.46.4pKd1
Homo sapiensSPS1/STE20-related protein kinase YSK48.38.38.3pKd1
Homo sapiensStem cell growth factor receptor8.28.28.4pIC506
Homo sapiensStem cell growth factor receptor8.57.48.7pKd8
Homo sapiensTRAF2- and NCK-interacting kinase6.76.76.7pKd1
Homo sapiensTyrosine kinase non-receptor protein 26.76.76.7pKd1
Homo sapiensTyrosine-protein kinase ABL7.46.58.4pKd15
Homo sapiensTyrosine-protein kinase ABL27.67.67.6pKd1
Homo sapiensTyrosine-protein kinase BLK8.38.38.3pKd1
Homo sapiensTyrosine-protein kinase BMX6.76.76.7pKd1
Homo sapiensTyrosine-protein kinase BRK8.48.48.4pKd1
Homo sapiensTyrosine-protein kinase BTK7.17.17.1pKd1
Homo sapiensTyrosine-protein kinase CSK6.96.96.9pKd1
Homo sapiensTyrosine-protein kinase FER7.47.47.4pKd1
Homo sapiensTyrosine-protein kinase FES777pKd1
Homo sapiensTyrosine-protein kinase FGR7.47.47.4pKd1
Homo sapiensTyrosine-protein kinase FRK8.48.48.4pKd1
Homo sapiensTyrosine-protein kinase FYN7.17.17.1pKd1
Homo sapiensTyrosine-protein kinase HCK7.87.87.8pKd1
Homo sapiensTyrosine-protein kinase ITK/TSK7.27.27.2pKd1
Homo sapiensTyrosine-protein kinase JAK25.85.85.8pKd2
Homo sapiensTyrosine-protein kinase LCK8.28.28.2pKd1
Homo sapiensTyrosine-protein kinase Lyn888pKd1
Homo sapiensTyrosine-protein kinase receptor FLT38.38.38.4pIC505
Homo sapiensTyrosine-protein kinase receptor FLT38.889.1pKd8
Homo sapiensTyrosine-protein kinase receptor RET8.88.69.2pKd4
Homo sapiensTyrosine-protein kinase receptor Tie-19.19.19.1pKd1
Homo sapiensTyrosine-protein kinase receptor TYRO38.78.78.7pKd1
Homo sapiensTyrosine-protein kinase receptor UFO888pIC501
Homo sapiensTyrosine-protein kinase receptor UFO101010pKd1
Homo sapiensTyrosine-protein kinase SRC7.77.77.7pKd1
Homo sapiensTyrosine-protein kinase Srms7.87.87.8pKd1
Homo sapiensTyrosine-protein kinase SYK6.66.66.6pKd1
Homo sapiensTyrosine-protein kinase TEC6.56.56.5pKd1
Homo sapiensTyrosine-protein kinase TIE-2999pIC501
Homo sapiensTyrosine-protein kinase TIE-28.58.58.5pKd1
Homo sapiensTyrosine-protein kinase TXK6.36.36.3pKd1
Homo sapiensTyrosine-protein kinase TYK25.35.35.3pKd2
Homo sapiensTyrosine-protein kinase YES7.37.37.3pKd1
Homo sapiensVascular endothelial growth factor receptor 18.28.29.1pIC503
Homo sapiensVascular endothelial growth factor receptor 18.48.48.4pKd1
Homo sapiensVascular endothelial growth factor receptor 29.17.89.1pIC5014
Homo sapiensVascular endothelial growth factor receptor 27.97.97.9pKd1
Homo sapiensVascular endothelial growth factor receptor 38.68.68.6pIC503
Homo sapiensVascular endothelial growth factor receptor 38.88.88.8pKd1


Kinase-ligand interaction pattern
Hydrophobic Aromatic face-to-face Aromatic face-to-edge H-bond donor H-bond acceptor Ionic positive Ionic negative
I g.l II III αC
1 K
617
2 V
618
3 I
619
4 G
620
5 A
621
6 G
622
7 E
623
8 F
624
9 G
625
10 E
626
11 V
627
12 Y
628
13 K
629
14 V
643
15 A
644
16 I
645
17 K
646
18 T
647
19 L
648
20 D
659
αC b.l IV
21 F
660
22 L
661
23 G
662
24 E
663
25 A
664
26 G
665
27 I
666
28 M
667
29 G
668
30 Q
669
31 F
670
32 S
671
33 H
673
34 N
674
35 I
675
36 I
676
37 R
677
38 L
678
39 E
679
40 G
680
IV V GK hinge linker αD αE
41 V
681
42 M
689
43 I
690
44 I
691
45 T
692
46 E
693
47 Y
694
48 M
695
49 E
696
50 N
697
51 G
698
52 A
699
53 L
700
54 D
701
55 K
702
56 F
703
57 L
704
58 R
705
59 E
706
60 Y
729
αE VI c.l VII VIII x
61 L
730
62 A
731
63 N
732
64 M
733
65 N
734
66 Y
735
67 V
736
68 H
737
69 R
738
70 D
739
71 L
740
72 A
741
73 A
742
74 R
743
75 N
744
76 I
745
77 L
746
78 V
747
79 V
755
80 S
756
DFG a.l
81 D
757
82 F
758
83 G
759
84 L
760
85 S
761

Interaction pattern search
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