KLIFS - the kinase structures database

Version: 3.2
Updated: 29-Oct-2025

Kinase structure
Kinase:	EPHA2 (EphA2)
Family:	Eph
Group:	TK
Species:	HUMAN
IUPHAR/BPS ID:	1822
PDB:	5IA1
sc-PDB:
KIDFamMap:	Search
Release date:	2016-11-09
PubMed:	27768280
Chain:	A
Orthosteric ligand:	ZZL

Structural information
DFG conformation:	in
αC-helix conformation:	in
G-rich loop angle (distance):	62.9° (19Å)
G-rich loop rotation:	75.5°
Quality Score:	8
Resolution:	2.04 Å
Missing Residues:	0
Missing Atoms:	0

Ligand binding mode
Pockets	Subpockets	Waters
front		Cluster I1	Ligand Yes	Protein Yes

Pocket alignment
Uniprot sequence:	KVIGAGEFGEVYKVAIKTLDFLGEAGIMGQFSHNIIRLEGVMIITEYMENGALDKFLREYLANMNYVHRDLAARNILVVSDFGLS
Sequence structure:	KVIGAGEFGEVYKVAIKTLDFLGEAGIMGQFSHNIIRLEGVMIITEYMENGALDKFLREYLANMNYVHRDLAARNILVVSDFGLS

Ligand affinity
ChEMBL ID:	CHEMBL259084
Bioaffinities:	189 records for 71 kinases

Species	Kinase (ChEMBL naming)	Median	Min	Max	Type	Records
Homo sapiens	3-phosphoinositide dependent protein kinase-1	6.1	6.1	6.1	pKi	1
Homo sapiens	Casein kinase II alpha	4.7	4.7	4.7	pIC50	1
Homo sapiens	Casein kinase II alpha	5.4	5.4	5.4	pKi	1
Homo sapiens	Death-associated protein kinase 2	5	5	5	pKd	1
Homo sapiens	Dual specificity protein kinase CLK2	5.5	5.5	5.5	pKd	2
Homo sapiens	Dual specificity protein kinase CLK3	5.6	5.6	5.6	pKd	2
Homo sapiens	Dual specificity protein kinase CLK4	5.6	5.6	5.6	pKi	1
Homo sapiens	Ephrin type-A receptor 1	5.8	5.8	5.8	pKd	2
Homo sapiens	Ephrin type-A receptor 2	6.4	6.4	6.4	pKd	2
Homo sapiens	Ephrin type-A receptor 2	6.9	6.9	6.9	pKi	1
Homo sapiens	Ephrin type-A receptor 3	5.7	5.7	5.7	pKd	2
Homo sapiens	Ephrin type-A receptor 4	6.4	6.4	6.4	pKd	2
Homo sapiens	Ephrin type-A receptor 5	5.9	5.9	5.9	pKd	2
Homo sapiens	Ephrin type-A receptor 6	6.2	6.2	6.2	pKd	2
Homo sapiens	Ephrin type-A receptor 7	6	6	6	pKd	2
Homo sapiens	Ephrin type-B receptor 1	6.5	6.5	6.5	pKd	2
Homo sapiens	Ephrin type-B receptor 3	5.5	5.5	5.5	pKd	2
Homo sapiens	Ephrin type-B receptor 4	6.3	6.3	6.3	pKd	2
Homo sapiens	Epidermal growth factor receptor erbB1	5.2	5.2	5.5	pKd	4
Homo sapiens	Epidermal growth factor receptor erbB1	6.3	6.3	6.3	pKi	1
Homo sapiens	Epithelial discoidin domain-containing receptor 1	5.4	5.4	5.4	pKd	2
Homo sapiens	Fibroblast growth factor receptor 1	5.6	5.6	5.6	pKd	2
Homo sapiens	Fibroblast growth factor receptor 1	6	6	6	pKi	1
Homo sapiens	Fibroblast growth factor receptor 2	5.8	5.8	5.8	pKd	2
Homo sapiens	Fibroblast growth factor receptor 3	5.9	5.9	5.9	pKd	4
Homo sapiens	Fibroblast growth factor receptor 3	6.3	6.3	6.3	pKi	1
Homo sapiens	Focal adhesion kinase 1	5.5	5.5	5.5	pKi	1
Homo sapiens	G protein-coupled receptor kinase 5	6	6	6	pKi	1
Homo sapiens	Interleukin-1 receptor-associated kinase 3	5.9	5.9	5.9	pKd	2
Homo sapiens	MAP kinase-activated protein kinase 5	8.1	8.1	8.1	pKd	1
Homo sapiens	MAP kinase signal-integrating kinase 2	7.9	7.9	7.9	pIC50	1
Homo sapiens	Maternal embryonic leucine zipper kinase	6	6	6	pKi	1
Homo sapiens	Non-receptor tyrosine-protein kinase TNK1	5.6	5.6	5.6	pKd	2
Homo sapiens	NT-3 growth factor receptor	5.6	5.6	5.6	pKi	1
Homo sapiens	Platelet-derived growth factor receptor alpha	6.1	6.1	6.1	pIC50	1
Homo sapiens	Protein tyrosine kinase 2 beta	5.7	5.7	5.7	pKd	2
Homo sapiens	Proto-oncogene tyrosine-protein kinase MER	6.1	6.1	6.1	pKd	2
Homo sapiens	Proto-oncogene tyrosine-protein kinase ROS	5.5	5.5	5.5	pKd	2
Homo sapiens	Proto-oncogene tyrosine-protein kinase ROS	6.1	6.1	6.1	pKi	1
Homo sapiens	Ribosomal protein S6 kinase alpha 1	5.3	5.3	5.3	pKd	2
Homo sapiens	Serine/threonine-protein kinase 10	5.4	5.4	5.4	pKd	2
Mus musculus	Serine/threonine-protein kinase 12	6.8	6.8	6.8	pIC50	3
Homo sapiens	Serine/threonine-protein kinase 17A	6.7	6.7	6.7	pKd	2
Homo sapiens	Serine/threonine-protein kinase 17B	8.1	8.1	8.1	pKd	2
Homo sapiens	Serine/threonine-protein kinase Aurora-A	7.5	6.5	9	pIC50	10
Homo sapiens	Serine/threonine-protein kinase Aurora-A	8.7	8.2	9.5	pKd	7
Mus musculus	Serine/threonine-protein kinase Aurora-A	8.4	7.5	8.4	pIC50	4
Mus musculus	Serine/threonine-protein kinase Aurora-A	8.2	8.2	8.2	pKi	1
Homo sapiens	Serine/threonine-protein kinase Aurora-B	5.4	5.2	8	pIC50	7
Homo sapiens	Serine/threonine-protein kinase Aurora-B	7.4	7.4	7.4	pKd	2
Homo sapiens	Serine/threonine-protein kinase Aurora-C	7.6	7.6	7.6	pKd	2
Homo sapiens	Serine/threonine-protein kinase Chk2	4.6	4.6	4.6	pIC50	1
Homo sapiens	Serine/threonine-protein kinase Chk2	5.7	5.7	5.7	pKi	1
Homo sapiens	Serine/threonine-protein kinase PAK 1	5	5	5	pKi	1
Homo sapiens	Serine/threonine-protein kinase PLK1	4.3	4.3	4.3	pIC50	1
Homo sapiens	Serine/threonine-protein kinase PLK3	5.2	5.2	5.2	pKi	1
Homo sapiens	Serine/threonine-protein kinase PLK4	6.4	6.4	6.4	pKd	2
Homo sapiens	Serine/threonine-protein kinase SIK1	5.8	5.8	5.8	pKd	2
Homo sapiens	Tyrosine-protein kinase ABL	6.1	5.4	6.4	pKd	18
Homo sapiens	Tyrosine-protein kinase ABL	6.8	6.8	6.8	pKi	1
Homo sapiens	Tyrosine-protein kinase ABL2	5.5	5.5	5.5	pKd	2
Homo sapiens	Tyrosine-protein kinase BLK	7.2	7.2	7.2	pKd	3
Homo sapiens	Tyrosine-protein kinase BLK	7.1	7.1	7.1	pKi	1
Homo sapiens	Tyrosine-protein kinase BMX	5.5	5.5	5.5	pKd	2
Homo sapiens	Tyrosine-protein kinase BTK	5.4	5.4	5.4	pKd	2
Homo sapiens	Tyrosine-protein kinase BTK	5.6	5.6	5.6	pKi	1
Homo sapiens	Tyrosine-protein kinase CSK	5.1	5.1	5.1	pKd	2
Homo sapiens	Tyrosine-protein kinase FER	5.4	5.4	5.4	pKd	2
Homo sapiens	Tyrosine-protein kinase FGR	6.7	6.7	6.7	pKd	2
Homo sapiens	Tyrosine-protein kinase FYN	5.9	5.9	5.9	pKd	2
Homo sapiens	Tyrosine-protein kinase HCK	5.8	5.8	5.8	pKd	2
Homo sapiens	Tyrosine-protein kinase HCK	6.2	6.2	6.2	pKi	1
Homo sapiens	Tyrosine-protein kinase LCK	5.5	5.5	5.5	pIC50	1
Homo sapiens	Tyrosine-protein kinase LCK	6.2	6.2	6.2	pKd	2
Homo sapiens	Tyrosine-protein kinase LCK	5.7	5.7	5.7	pKi	1
Homo sapiens	Tyrosine-protein kinase Lyn	5.9	5.9	5.9	pKd	2
Homo sapiens	Tyrosine-protein kinase Lyn	6.6	6.6	6.6	pKi	1
Homo sapiens	Tyrosine-protein kinase receptor FLT3	5	5	5	pKd	1
Homo sapiens	Tyrosine-protein kinase receptor Tie-1	5.8	5.8	5.8	pKd	2
Homo sapiens	Tyrosine-protein kinase receptor TYRO3	5.5	5.5	5.5	pKd	2
Homo sapiens	Tyrosine-protein kinase receptor TYRO3	6.9	6.9	6.9	pKi	1
Homo sapiens	Tyrosine-protein kinase receptor UFO	6.4	6.4	6.4	pKd	2
Homo sapiens	Tyrosine-protein kinase SRC	6.1	6.1	6.1	pKd	2
Homo sapiens	Tyrosine-protein kinase SRC	5.8	5.8	5.8	pKi	1
Homo sapiens	Tyrosine-protein kinase TEC	6.1	6.1	6.1	pKd	2
Homo sapiens	Tyrosine-protein kinase TIE-2	6.5	6.5	6.5	pKd	2
Homo sapiens	Tyrosine-protein kinase YES	6.6	6.6	6.6	pKd	2
Homo sapiens	Vascular endothelial growth factor receptor 1	6	6	6	pKd	2
Homo sapiens	Vascular endothelial growth factor receptor 2	6.1	6.1	6.1	pKi	1
Homo sapiens	Vascular endothelial growth factor receptor 3	5.5	5.5	5.5	pKd	2
Homo sapiens	Vascular endothelial growth factor receptor 3	6.3	6.3	6.3	pKi	1

Kinase-ligand interaction pattern

• Hydrophobic • Aromatic face-to-face • Aromatic face-to-edge • H-bond donor • H-bond acceptor • Ionic positive • Ionic negative

g.l

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

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

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

c.l

VII

VIII

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

Search KLIFS for kinase-ligand complexes with similar interaction patterns: