The Ligandable Human Proteome

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Coagulation factor X

Serine proteases, trypsin domain

IndexLigand NameStructurePDB codeCompound Potency nM
1xldCrystal 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 Xa1mq60.007
2lg0FACTOR 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)-one3cs70.021
35qcFactor 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-one2fzz0.03
4iibCrystal structure of factor Xa in complex with 212bq60.07
5l1dCrystal Structure of FXa in complex with 4,4-disubstituted pyrrolidine-1,2-dicarboxamide inhibitor 12w3k0.08
6gg2Factor 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-CARBOXAMIDE2p160.08
7l1cCrystal Structure of FXa in complex with 4,4-disubstituted pyrrolidine-1,2-dicarboxamide inhibitor 22w3i0.1
8z34CRYSTAL STRUCTURE OF THE INHIBITOR ZK-807834 (CI-1031) COMPLEXED WITH FACTOR XA1fjs0.11
94qcFactor 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)benzamide2g000.18
10ik8Factor 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)1z6e0.19
11230An Orally Efficacious Factor Xa Inhibitor2phb0.32
12lglFactor 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)-one3kqd0.4
13fxvCrystal Structure of Human Coagulation Factor XA Complexed with FXV6731ksn0.4
14rivFactor Xa in complex with BAY59-79392w260.4
15me5Factor xa in complex with the inhibitor 5-chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-YL)benzamido) cyclopentyl)thiophene-2-carboxamide2p950.43
16me4Factor xa in complex with the inhibitor 3-chloro-N-((1R,2S)-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)cyclohexyl)-1H-indole-6-carboxamide2p940.67
17fxiThe discovery of glycine and related amino acid-based factor xa inhibitors2q1j0.8
18ffgFactor 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)-ONE3ffg0.84
19rprCRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR1285151ezq0.9
20xlcCrystal 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 Xa1mq51
21gsjCRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX2j4i1
22898Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs2wyj1
23rrrCRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR2096851nfw1.1
24rtrCRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR2000951nfy1.3
25me1Factor xa in complex with the inhibitor 5-chloro-N-(2-(4-(2-oxopyridin-1(2H)-yl)benzamido)ethyl)thiophene-2-carboxamide2p931.5
26xwgFACTOR XA - CATION INHIBITOR COMPLEX2y5f2
27701Selective and Dual Action Orally Active Inhibitors of Thrombin and Factor Xa2uwo2
28461Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs2wyg2
29a7iFactor Xa in complex with a potent 2-amino-ethane sulfonamide inhibitor4a7i2
30rdrCRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR2089441nfx3
31lzfAminopyrrolidine Factor Xa inhibitor2vvc3
32iiaCrystal structure of factor Xa in complex with compound ""1""2boh3
33iieCRYSTAL STRUCTURE OF FACTOR XA IN COMPLEX WITH COMPOUND 452bqw3
34gsiStructure and property based design of factor Xa inhibitors:biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs2vh03.1
35443Discovery of Tetrahydropyrimidin-2(1H)-one derivative TAK-442: A potent, selective and orally active factor Xa inhibitor3kl63.5
36xbvFactor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor2xbv3.7
37mbmX-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)NICOTINAMIDE3k9x4
38gsxCRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX2j954
39895Selective and Dual Action Orally Active Inhibitors of Thrombin and Factor Xa2uwl4
40fi1X-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-sulfonamide3sw24.71
41gskCrystal structure of a Human Factor Xa inhibitor complex2cji6
42h21Aminopyrrolidine-related triazole Factor Xa inhibitor2vvv6
43yetCrystal 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)guanidine3hpt6.5
44d90Factor Xa in complex with a phenylenediamine derivative3q3k7.4
45h22Aminopyrrolidine Factor Xa inhibitor2vvu8
46lgmFactor 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)-one3kqe8.1
47ensCrystal 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}acrylate3ens8.9
48ivkFactor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor2xc49
49bi7Factor Xa - cation inhibitor complex2jkh9
50d14Factor XA in complex with a cis-1,2-diaminocyclohexane derivative3iit9.5
51455Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor2xbw10
52h25Aminopyrrolidine Factor Xa inhibitor2vwn10
534o6Factor Xa complex with GTC0004064y7911
54rr8Factor Xa in complex with a pyrrolidine-3,4-dicarboxylic acid inhibitor2xbx15
55gs6CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX2j3415
56jnjX-ray Structure of FXa in complex with 7-fluoroindazole2ra015.9
57i1hCrystal structure of factor Xa in complex with 502bmg18
58d91Factor Xa in complex with the inhibitor 4-[(5-chloroindol-2-yl)sulfonyl]-2-(2-methylpropyl)-1-[[5-(pyridin-4-yl) pyrimidin-2-yl]carbonyl]piperazine1wu118
59pr2Crystal Structure of Human Coagulation Factor XA Complexed with RPR2087071f0s18
60rrpCRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR1327471nfu18
61815CRYSTAL STRUCTURE OF HUMAN COAGULATION FACTOR XA COMPLEXED WITH RPR2088151f0r22
62d76Factor 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)piperazine1v3x24
63lzgAminopyrrolidine Factor Xa inhibitor2vwo31
64dx9COAGULATION FACTOR XA INHIBITOR COMPLEX1fax41
65d92FACTOR 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-cyclohexanediamine2ei641
66gsqCRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX2j2u47
67t87FACTOR XA INHIBITOR COMPLEX1g2l57
68iidCrystal structure of factor Xa in complex with 432bq789
69lziAminopyrrolidine Factor Xa inhibitor2vwm93
70lzhAminopyrrolidine Factor Xa inhibitor2vwl95
714ppFACTOR XA COMPLEXED WITH A SYNTHETIC INHIBITOR FX-2212A,(2S)-(3'-AMIDINO-3-BIPHENYLYL)-5-(4-PYRIDYLAMINO)PENTANOIC ACID1xka131
72fjdFACTOR XA - CATION INHIBITOR COMPLEX2y5g146
73894Factor Xa inhibitor complex2uwp154
74784Factor Xa - cation2bok280
75g15CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX2j94534
76y5hFACTOR XA - CATION INHIBITOR COMPLEX2y5h1620