The Ligandable Human Proteome

Coagulation factor X

Index	Ligand Name	Structure	PDB code	ligand desolvation
1	443	Discovery of Tetrahydropyrimidin-2(1H)-one derivative TAK-442: A potent, selective and orally active factor Xa inhibitor	3kl6	84.52
2	a7i	Factor Xa in complex with a potent 2-amino-ethane sulfonamide inhibitor	4a7i	83.1
3	h25	Aminopyrrolidine Factor Xa inhibitor	2vwn	82.91
4	lzg	Aminopyrrolidine Factor Xa inhibitor	2vwo	82.33
5	455	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xbw	82
6	d46	factor Xa in complex with D46-5241	3tk6	81.77
7	riv	Factor Xa in complex with BAY59-7939	2w26	81.62
8	me5	Factor xa in complex with the inhibitor 5-chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-YL)benzamido) cyclopentyl)thiophene-2-carboxamide	2p95	81.51
9	lzh	Aminopyrrolidine Factor Xa inhibitor	2vwl	81.39
10	xbv	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xbv	81.17
11	riv	DesGla-XaS195A Bound to Aptamer 11F7t and Rivaroxaban	5vof	81.09
12	784	Factor Xa - cation	2bok	80.76
13	lzf	Aminopyrrolidine Factor Xa inhibitor	2vvc	80.66
14	iia	Crystal structure of factor Xa in complex with compound ""1""	2boh	80.43
15	d90	Factor Xa in complex with a phenylenediamine derivative	3q3k	80.32
16	rrr	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR209685	1nfw	80.25
17	701	Selective and Dual Action Orally Active Inhibitors of Thrombin and Factor Xa	2uwo	80.09
18	rtr	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR200095	1nfy	79.85
19	iib	Crystal structure of factor Xa in complex with 21	2bq6	79.84
20	iie	CRYSTAL STRUCTURE OF FACTOR XA IN COMPLEX WITH COMPOUND 45	2bqw	79.83
21	ivk	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xc4	79.78
22	oyj	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xc5	79.78
23	4o5	Factor Xa complex with GTC000102	4zha	79.75
24	h21	Aminopyrrolidine-related triazole Factor Xa inhibitor	2vvv	79.62
25	fxv	Crystal Structure of Human Coagulation Factor XA Complexed with FXV673	1ksn	79.5
26	48u	Factor Xa complex with GTC000101	4y6d	79.33
27	d91	Factor Xa in complex with the inhibitor 4-[(5-chloroindol-2-yl)sulfonyl]-2-(2-methylpropyl)-1-[[5-(pyridin-4-yl) pyrimidin-2-yl]carbonyl]piperazine	1wu1	79.31
28	rr8	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xbx	79.27
29	me1	Factor xa in complex with the inhibitor 5-chloro-N-(2-(4-(2-oxopyridin-1(2H)-yl)benzamido)ethyl)thiophene-2-carboxamide	2p93	79.25
30	fjd	FACTOR XA - CATION INHIBITOR COMPLEX	2y5g	79.06
31	d93	FACTOR XA IN COMPLEX WITH THE INHIBITOR trans-N1-[(5-Chloroindol-2-yl)carbonyl]-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine	2ei7	78.87
32	gg2	Factor Xa in Complex with the Inhibitor APIXABAN (BMS-562247) AKA 1-(4-METHOXYPHENYL)-7-OXO-6-(4-(2-OXO-1-PIPERIDINYL)PHENYL)-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[3, 4-C]PYRIDINE-3-CARBOXAMIDE	2p16	78.83
33	d01	Factor Xa in complex with the inhibitor 2-[[4-[(5-chloroindol-2-yl)sulfonyl]piperazin-1-yl] carbonyl]thieno[3,2-b]pyridine n-oxide	2d1j	78.79
34	h22	Aminopyrrolidine Factor Xa inhibitor	2vvu	78.74
35	gsq	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j2u	78.73
36	63c	Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor	2xby	78.69
37	663	Crystal structure of human factor XA complexed with 3-chloro-N-(4-chloro-2-{[(5-chloropyridin-2-yl)amino]carbonyl}-6-methoxyphenyl)-4-[(1-methyl-1H-imidazol-2-yl)methyl]thiophene-2-carboxamide {Pfizer 320663}	2p3u	78.44
38	gsk	Crystal structure of a Human Factor Xa inhibitor complex	2cji	78.4
39	iid	Crystal structure of factor Xa in complex with 43	2bq7	78.37
40	4pp	FACTOR XA COMPLEXED WITH A SYNTHETIC INHIBITOR FX-2212A,(2S)-(3'-AMIDINO-3-BIPHENYLYL)-5-(4-PYRIDYLAMINO)PENTANOIC ACID	1xka	78.27
41	xlc	Crystal Structure of 3-chloro-N-[4-chloro-2-[[(4-chlorophenyl)amino]carbonyl]phenyl]-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide Complexed with Human Factor Xa	1mq5	78.26
42	4o6	Factor Xa complex with GTC000406	4y79	78.17
43	g15	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j94	78.11
44	894	Factor Xa inhibitor complex	2uwp	78.06
45	yet	Crystal structure of human FxA in complex with (S)-2-cyano-1-(2-methylbenzofuran-5-yl)-3-(2-oxo-1-(2-oxo-2-(pyrrolidin-1-yl)ethyl)azepan-3-yl)guanidine	3hpt	77.94
46	l1c	Crystal Structure of FXa in complex with 4,4-disubstituted pyrrolidine-1,2-dicarboxamide inhibitor 2	2w3i	77.94
47	gsx	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j95	77.89
48	gs6	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j34	77.84
49	895	Selective and Dual Action Orally Active Inhibitors of Thrombin and Factor Xa	2uwl	77.59
50	gs5	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j38	77.47
51	987	Factor Xa complex with GTC000422	4y7a	77.33
52	l1d	Crystal Structure of FXa in complex with 4,4-disubstituted pyrrolidine-1,2-dicarboxamide inhibitor 1	2w3k	77.27
53	230	An Orally Efficacious Factor Xa Inhibitor	2phb	77.12
54	4pp	FACTOR XA COMPLEXED WITH A SYNTHETIC INHIBITOR FX-2212A,(2S)-(3'-AMIDINO-3-BIPHENYLYL)-5-(4-PYRIDYLAMINO)PENTANOIC ACID	1xkb	77
55	i1h	Crystal structure of factor Xa in complex with 50	2bmg	76.88
56	xmj	Human coagulation factor Xa in complex with M54476	1iql	76.82
57	y5h	FACTOR XA - CATION INHIBITOR COMPLEX	2y5h	76.82
58	xme	Human coagulation factor Xa in complex with M55159	1iqg	76.75
59	xmg	Human coagulation factor Xa in complex with M55125	1iqi	76.74
60	rpr	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR128515	1ezq	76.72
61	ik8	Factor XA in complex with the inhibitor 1-(3'-amino-1,2-benzisoxazol-5'-yl)-n-(4-(2'-((dimethylamino)methyl)-1h-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazole-5-carboxamide (razaxaban; DPC906; BMS-561389)	1z6e	76.66
62	48w	Factor Xa complex with GTC000398	4y71	76.57
63	bi7	Factor Xa - cation inhibitor complex	2jkh	76.56
64	d1q	Factor Xa in complex with D102-4380	3tk5	76.44
65	pr2	Crystal Structure of Human Coagulation Factor XA Complexed with RPR208707	1f0s	76.4
66	d76	Factor Xa in complex with the inhibitor 1-[6-methyl-4,5,6,7-tetrahydrothiazolo(5,4-c)pyridin-2-yl] carbonyl-2-carbamoyl-4-(6-chloronaphth-2-ylsulphonyl)piperazine	1v3x	76.38
67	xmf	Human coagulation factor Xa in complex with M55143	1iqh	76.37
68	ens	Crystal structure of human FXA in complex with methyl (2Z)-3-[(3-chloro-1H-indol-7-yl)amino]-2-cyano-3-{[(3S)-2-oxo-1-(2-oxo-2-pyrrolidin-1-ylethyl)azepan-3-yl]amino}acrylate	3ens	75.94
69	4qc	Factor Xa in complex with the inhibitor 3-(6-(2'-((dimethylamino)methyl)-4-biphenylyl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl)benzamide	2g00	75.71
70	xwg	FACTOR XA - CATION INHIBITOR COMPLEX	2y5f	75.49
71	898	Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs	2wyj	75.46
72	me4	Factor xa in complex with the inhibitor 3-chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)cyclohexyl)-1H-indole-6-carboxamide	2p94	75.27
73	rrp	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR132747	1nfu	75.23
74	fxi	The discovery of glycine and related amino acid-based factor xa inhibitors	2q1j	75.05
75	xld	Crystal Structure of 3-chloro-N-[4-chloro-2-[[(5-chloro-2-pyridinyl)amino]carbonyl]-6-methoxyphenyl]-4-[[(4,5-dihydro-2-oxazolyl)methylamino]methyl]-2-thiophenecarboxamide Complexed with Human Factor Xa	1mq6	74.99
76	461	Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs	2wyg	74.84
77	jnj	X-ray Structure of FXa in complex with 7-fluoroindazole	2ra0	74.51
78	lg0	FACTOR XA IN COMPLEX WITH THE INHIBITOR 1-(4-methoxyphenyl)-6-(4-(1-(pyrrolidin-1-ylmethyl)cyclopropyl)phenyl)-3-(trifluoromethyl)-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one	3cs7	74.5
79	993	Crystal structure of human factor XA complexed with 3-Chloro-4-(2-methylamino-imidazol-1-ylmethyl)-thiophene-2-carboxylic acid [4-chloro-2-(5-chloro-pyridin-2-ylcarbamoyl)-6-methoxy-phenyl]-amide	2p3t	74.47
80	lgl	Factor xa in complex with the inhibitor 1-(3-(5-oxo-4,5- dihydro-1h-1,2,4-triazol-3-yl)phenyl)-6-(2'-(pyrrolidin-1- ylmethyl)biphenyl-4-yl)-3-(trifluoromethyl)-5,6-dihydro- 1h-pyrazolo[3,4-c]pyridin-7(4h)-one	3kqd	74.46
81	lzi	Aminopyrrolidine Factor Xa inhibitor	2vwm	74.43
82	d92	FACTOR XA IN COMPLEX WITH THE INHIBITOR (-)-cis-N1-[(5-Chloroindol-2-yl)carbonyl]-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine	2ei6	74.42
83	815	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR208815	1f0r	74.19
84	rdr	CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR208944	1nfx	74.18
85	xmk	Human coagulation factor Xa in complex with M54471	1iqm	74.09
86	gsi	Structure and property based design of factor Xa inhibitors:biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs	2vh0	73.74
87	d14	Factor XA in complex with a cis-1,2-diaminocyclohexane derivative	3iit	73.73
88	237	Factor XA inhibitor	2pr3	73.3
89	dx9	COAGULATION FACTOR XA INHIBITOR COMPLEX	1fax	73.16
90	lgm	Factor xa in complex with the inhibitor 3-methyl-1-(3-(5- oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl)phenyl)-6-(2'- (pyrrolidin-1-ylmethyl)biphenyl-4-yl)-5,6-dihydro-1h- pyrazolo[3,4-c]pyridin-7(4h)-one	3kqe	73.08
91	fi1	X-ray crystal structure of human FXA in complex with 6-chloro-N-((3S)-2-oxo-1-(2-oxo-2-((5S)-8-oxo-5,6-dihydro-1H-1,5-methanopyrido[1,2-a][1,5]diazocin-3(2H,4H,8H)-yl)ethyl)piperidin-3-yl)naphthalene-2-sulfonamide	3sw2	72.29
92	xma	Human coagulation factor Xa in complex with M55532	1ioe	72.25
93	gsj	CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX	2j4i	72.04
94	ffg	Factor XA in complex with the inhibitor (R)-6-(2'-((3- HYDROXYPYRROLIDIN-1-YL)METHYL)BIPHENYL-4-YL)-1-(3-(5-OXO-4,5-DIHYDRO-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3-(TRIFLUOROMETHYL)-5,6-DIHYDRO-1H-PYRAZOLO[3,4-C]PYRIDIN- 7(4H)-ONE	3ffg	71.98
95	t87	FACTOR XA INHIBITOR COMPLEX	1g2l	71.73
96	4o4	Factor Xa complex with GTC000006	4zh8	71.72
97	mbm	X-ray crystal structure of human fxa in complex with (S)-N-((2-METHYLBENZOFURAN-5-YLAMINO)(2-OXO-1-(2-OXO-2- (PYRROLIDIN-1-YL)ETHYL)AZEPAN-3- YLAMINO)METHYLENE)NICOTINAMIDE	3k9x	71.68
98	z34	CRYSTAL STRUCTURE OF THE INHIBITOR ZK-807834 (CI-1031) COMPLEXED WITH FACTOR XA	1fjs	71.45
99	44i	Factor Xa complex with GTC000441	4y7b	71.36
100	5qc	Factor Xa in complex with the inhibitor 1-(3-amino-1,2-benzisoxazol-5-yl)-6-(2'-(((3r)-3-hydroxy-1-pyrrolidinyl)methyl)-4-biphenylyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7h-pyrazolo[3,4-c]pyridin-7-one	2fzz	71.33
101	4o1	Factor Xa complex with GTC000401	4y76	70.08
102	xmh	Human coagulation factor Xa in complex with M55124	1iqj	70.05
103	dt8	FACTOR XA IN COMPLEX WITH THE INHIBITOR (1S,2R,4S)-N1-[(5-chloroindol-2-yl)carbonyl]-4-(N,N-dimethylcarbamoyl)-N2-[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]-1,2-cyclohexanediamine	2ei8	67.02