The Ligandable Human Proteome

Mitogen-activated protein kinase 1

Index	Ligand Name	Structure	PDB code	ligand desolvation
1	g17	Crystal Structure of a Double Mutant Rat Erk2 Complexed With a Type II Quinazoline Inhibitor	4i5h	96
2	4vb	ERK2 complexed with a N-H tetrahydroazaindazole	5buj	95.37
3	4v9	ERK2 complexed with 2-pyridiyl tetrahydroazaindazole	5bui	94
4	2h1	A Double Mutant Rat Erk2 in Complex With a Pyrazolo[3,4-d]pyrimidine Inhibitor	4n4s	93.77
5	erk	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9j	91.93
6	8xh	Human Erk2 with an Erk1/2 inhibitor	5nhh	91.86
7	35x	Crystal Structure of ERK2 in complex with 7-(1-propyl-1H-pyrazol-4-yl)-2-(pyridin-4-yl)-5H-pyrrolo[2,3-b]pyrazine	4qp9	90.71
8	4vf	Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase	5bvd	90.24
9	1fm	The structure of ERK2 in complex with FR148083	3w55	89.51
10	ek9	Crystal Structure of the ERK2 complexed with EK9	4fv5	89.43
11	6qb	Crystal Structure of ERK2 in complex with compound 22	5k4i	89.35
12	82a	Crystal structure of ERK2 in complex with (S)-N-(1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl)-4-(4-(3-chlorophenyl)-1H-pyrazol-3-yl)-1H-pyrrole-2-carboxamide	2ojj	89.07
13	8xe	Human Erk2 with an Erk1/2 inhibitor	5nhj	88.93
14	f3z	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6gdm	88.85
15	38z	Structure of human ERK2 in complex with SCH772984 revealing a novel inhibitor-induced binding pocket	4qta	88.74
16	4vg	Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase	5bve	88.66
17	esk	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9k	88.23
18	eqz	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g97	88.12
19	e57	Crystal Structure of the ERK2 complexed with E57	4fv6	88.06
20	8qb	Human Erk2 with an Erk1/2 inhibitor	5nhv	88.02
21	3g7	Discovery of Novel, Dual Mechanism ERK Inhibitors by Affinity Selection Screening of an Inactive Kinase State	4qyy	87.86
22	esn	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9n	87.75
23	5id	Crystal structure of ERK2 complexed with allosteric and ATP-competitive inhibitors.	5ax3	87.63
24	e94	Crystal Structure of the ERK2 complexed with E94	4fv7	87.62
25	du8	Crystal structure of ERK2 in complex with an adenosine derivative	6fma	87.48
26	er8	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9d	87.36
27	390	Phosphorylated ERK2 with Vertex-11e	6opk	87.24
28	8xn	Human Erk2 with an Erk1/2 inhibitor	5nho	87.17
29	4v8	ERK2 complexed with N-benzylpyridone tetrahydroazaindazole	5bue	87.14
30	evq	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6ge0	86.99
31	4vj	Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase	5bvf	86.93
32	38z	Dissecting Therapeutic Resistance to ERK Inhibition Rat Wild Type SCH772984 in complex with (3R)-1-(2-oxo-2-{4-[4-(pyrimidin-2-yl)phenyl]piperazin-1-yl}ethyl)-N-[3-(pyridin-4-yl)-2H-indazol-5-yl]pyrrolidine-3-carboxamide	5hd4	86.82
33	e86	Crystal structure of ERK2 bound to (S)-4-(2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl)-N-(2-hydroxy-1-phenylethyl)-1H-pyrrole-2-carboxamide	3i60	86.75
34	6qb	phosphorylated ERK2 with GDC-0994	6oph	86.68
35	390	Structure of ERK2 in complex with VTX-11e, 4-{2-[(2-CHLORO-4-FLUOROPHENYL)AMINO]-5-METHYLPYRIMIDIN-4-YL}-N-[(1S)-1-(3-CHLOROPHENYL)-2-HYDROXYETHYL]-1H-PYRROLE-2-CARBOXAMIDE	4qte	86.66
36	ek7	Crystal Structure of the ERK2 complexed with EK7	4fv4	86.61
37	z48	Crystal structure of ERK2 bound to (S)-N-(2-hydroxy-1-phenylethyl)-4-(5-methyl-2-(phenylamino)pyrimidin-4-yl)-1H-pyrrole-2-carboxamide	3i5z	86.57
38	38z	Dissecting Therapeutic Resistance to ERK Inhibition Rat Mutant SCH772984 in complex with (3R)-1-(2-oxo-2-{4-[4-(pyrimidin-2-yl)phenyl]piperazin-1-yl}ethyl)-N-[3-(pyridin-4-yl)-2H-indazol-5-yl]pyrrolidine-3-carboxamide	5hd7	86.42
39	evk	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6gdq	86.13
40	cq3	Human ERK2 in complex with an irreversible inhibitor	4zzo	85.7
41	35w	Crystal Structure of ERK2 in complex with 7-(1-benzyl-1H-pyrazol-4-yl)-2-(pyridin-4-yl)-5H-pyrrolo[2,3-b]pyrazine	4qpa	85.69
42	z8b	Crystal structure of ERK2 in complex with an inhibitor	3qyz	85.66
43	n0v	phosphorylated ERK2 with SCH-CPD336	6opi	85.61
44	6tt	A Clickable Covalent ERK 1/2 Inhibitor	5lck	85.5
45	f8v	Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology	6cpw	85.42
46	erw	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9h	85.23
47	6s9	Discovery of 1-1H-Pyrazolo 4,3-c pyridine-6-yl urea Inhibitors of Extracellular Signal Regulated Kinase ERK for the Treatment of Cancers	5ke0	84.82
48	ek3	Crystal Structure of the ERK2 complexed with EK3	4fv0	84.29
49	ek5	Crystal Structure of the ERK2 complexed with EK5	4fv2	83.95
50	8xk	Human Erk2 with an Erk1/2 inhibitor	5nhp	83.86
51	zas	Crystal structure of ERK2 in complex with an adenosine derivative	6frp	83.85
52	8xb	Human Erk2 with an Erk1/2 inhibitor	5nhl	83.7
53	e2k	Crystal structure of ERK2 in complex with an adenosine derivative	6fq7	83.47
54	ek0	Crystal Structure of the ERK2	4g6n	82.79
55	8x5	Human Erk2 with an Erk1/2 inhibitor	5nhf	81.96
56	eu2	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g93	81.68
57	cq8	Human ERK2 in complex with an inhibitor	4zzn	81.4
58	ek6	A multiconformer ligand model of EK6 bound to ERK2	6dmg	81.34
59	2sh	Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine Inhibitors of Erk2	4o6e	81.25
60	esw	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9m	81.14
61	dj2	Crystal structure of ERK2 in complex with an adenosine derivative	6fi3	80.98
62	41b	Crystal structure of ERK2 in complex with an inhibitor 14K	4xj0	80.68
63	e63	Crystal Structure of the ERK2 complexed with E63	4fv8	80.27
64	e28	Crystal Structure of the ERK2	4g6o	79.59
65	ek6	Crystal Structure of the ERK2 complexed with EK6	4fv3	79.53
66	esq	Fragment-based discovery of a highly potent, orally bioavailable inhibitor which modulates the phosphorylation and catalytic activity of ERK1/2	6g9a	79
67	a3n	Crystal structure of ERK2 in complex with an adenosine derivative	6fj0	78.83
68	cq6	Human ERK2 in complex with an irreversible inhibitor	4zzm	78.36
69	sb4	THE COMPLEX STRUCTURE OF THE MAP KINASE ERK2/SB220025	3erk	78.31
70	aoc	Crystal structure of ERK2 in complex with an adenosine derivative	6fjb	78.08
71	36q	Crystal Structure of ERK2 in complex with (S)-2-((9H-purin-6-yl)amino)-3-phenylpropan-1-ol	4qp3	77.78
72	e75	Crystal Structure of the ERK2 complexed with E75	4fux	77.53
73	dkw	Crystal structure of ERK2 in complex with an adenosine derivative	6fjz	76.88
74	s91	Unphosphorylated Mitogen Activated Protein Kinase ERK2 in Complex with (4-{[5-Carbamoyl-4-(3-Methylanilino)Pyrimidin 2-Yl]Amino}Phenyl)Acetic Acid	2z7l	76.73
75	olo	THE COMPLEX STRUCTURE OF THE MAP KINASE ERK2/OLOMOUCINE	4erk	75.55
76	8x2	Human Erk2 with an Erk1/2 inhibitor	5ngu	75.45
77	6h3	Crystal structure of ERK2 covalently bound to SM1-71	6g54	75.34
78	6ts	In-Gel Activity-Based Protein Profiling of a Clickable Covalent Erk 1/2 Inhibitor	5lcj	54.2