General Information of the Protein
Protein ID
PT00868
Protein Name
Coagulation factor X
Secondarily
Protein Name
Stuart factor
Stuart-Prower factor
Gene Name
F10
Sequence
MGRPLHLVLLSASLAGLLLLGESLFIRREQANNILARVTRANSFLEEMKKGHLERECMEETCSYEEAREVFEDSDKTNEFWNKYKDGDQCETSPCQNQGKCKDGLGEYTCTCLEGFEGKNCELFTRKLCSLDNGDCDQFCHEEQNSVVCSCARGYTLADNGKACIPTGPYPCGKQTLERRKRSVAQATSSSGEAPDSITWKPYDAADLDPTENPFDLLDFNQTQPERGDNNLTRIVGGQECKDGECPWQALLINEENEGFCGGTILSEFYILTAAHCLYQAKRFKVRVGDRNTEQEEGGEAVHEVEVVIKHNRFTKETYDFDIAVLRLKTPITFRMNVAPACLPERDWAESTLMTQKTGIVSGFGRTHEKGRQSTRLKMLEVPYVDRNSCKLSSSFIITQNMFCAGYDTKQEDACQGDSGGPHVTRFKDTYFVTGIVSWGEGCARKGKYGIYTKVTAFLKWIDRSMKTRGLPKAKSHAPEVITSSPLK
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Serine protease
>
Serine protease PA clan
>
Serine protease S1A subfamily
Function
Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting.
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Uniprot ID
Primary ID:
P00742

Secondarily ID:
Q14340
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HGNC ID
HGNC:3528
Subcellular Location
Secreted
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0549332
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-[6-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-1,3-benzothiazol-2-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-(2-methylpropyl)-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C36H55N11O7S
  1
1
IC50 = 118 nM
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CP0355345
 Compound Info 
(2S,5S,14S)-14-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-[3-(diaminomethylideneamino)propyl]-3,8,15-trioxo-1,4,9-triazacyclopentadecane-5-carboxamide
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C32H48N12O6S
  1
1
IC50 = 155 nM
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CP0577980
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-9-methyl-3-(2-methylpropyl)-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C32H47N9O6S
  1
1
IC50 = 678 nM
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CP0343998
 Compound Info 
(2S,5S,14S)-14-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-(2-methylpropyl)-3,8,15-trioxo-1,4,9-triazacyclopentadecane-5-carboxamide
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C32H47N9O6S
  1
1
IC50 = 723 nM
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CP0260875
 Compound Info 
2-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]-6-aminohexanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]-1,3-benzothiazole-6-carboxamide
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C36H57N11O8S
  1
1
IC50 = 770 nM
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CP0540302
 Compound Info 
(2S,5S,13S)-13-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2-(2-methylpropyl)-3,7,14-trioxo-1,4,8-triazacyclotetradecane-5-carboxamide
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C31H45N9O6S
  1
1
IC50 = 1161 nM
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CP0572090
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-3-(2-methylpropyl)-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C27H43N9O6S
  1
1
IC50 = 1363 nM
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CP0554211
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-(2-methylsulfanylethyl)-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C30H43N9O6S2
  1
1
IC50 = 1395 nM
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CP0549331
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5,8-trioxo-3-propan-2-yl-1,4,9-triazacyclotetradecane-14-carboxamide
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C30H43N9O6S
  1
1
IC50 = 1514 nM
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CP0343999
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-benzyl-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C34H43N9O6S
  1
1
IC50 = 1530 nM
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CP0533742
 Compound Info 
(3S,6S,15S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-(2-methylpropyl)-2,5,8-trioxo-1,4,9-triazacyclopentadecane-15-carboxamide
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C32H47N9O6S
  1
1
IC50 = 1714 nM
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CP0549727
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-(2-methylpropyl)-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C31H45N9O6S
  1
1
IC50 = 2048 nM
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CP0571520
 Compound Info 
(3S,6S,14S)-6-acetamido-3-(2-amino-2-oxoethyl)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C29H40N10O7S
  1
1
IC50 = 4653 nM
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CP0549333
 Compound Info 
(6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C27H37N9O6S
  1
1
IC50 = 6183 nM
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CP0549334
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-[(1R)-1-hydroxyethyl]-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C29H41N9O7S
  1
1
IC50 = 13341 nM
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CP0579026
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-[(4-hydroxyphenyl)methyl]-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C34H43N9O7S
  1
1
IC50 = 16962 nM
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CP0260405
 Compound Info 
(3S,6S,14S)-6-acetamido-3-(3-amino-3-oxopropyl)-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C30H42N10O7S
  1
1
IC50 > 20000 nM
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CP0533744
 Compound Info 
(3S,6S,14S)-6-acetamido-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-3-methyl-2,5,8-trioxo-1,4,9-triazacyclotetradecane-14-carboxamide
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C28H39N9O6S
  1
1
IC50 > 20000 nM
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CP0063723
 Compound Info 
4-[(5-phenyl-1H-imidazol-2-yl)methylamino]-2-(pyridin-3-ylmethoxy)benzenecarboximidamide
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C23H22N6O
  1
1
IC50 > 100000 nM
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CP0658153
 Compound Info 
3-[[(5-chlorothiophene-2-carbonyl)amino]methyl]-N-[2-fluoro-4-(2-oxopyridin-1-yl)phenyl]-1,2,4-oxadiazole-5-carboxamide
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C20H13ClFN5O4S
  1
1
Kd = 5.003 nM
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CP0649829
 Compound Info 
5-chloro-N-[1-[2-[2-fluoro-4-(2-oxopyridin-1-yl)anilino]-2-oxoethyl]-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
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C23H22ClFN4O4S
  1
1
Kd = 5.397 nM
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CP0091693
 Compound Info 
BAY 59-7939 Analog 11
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C19H18ClN3O4S
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1
Kd = 5.645 nM
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CP0055905
 Compound Info 
BAY 59-7939 Analog 14
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C19H19ClN4O5S
  1
1
Kd = 7.16 nM
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CP0913970
 Compound Info 
5-chloro-N-[(3S,4R)-1-[2-[2-fluoro-4-(2-oxopyridin-1-yl)anilino]-2-oxoethyl]-4-hydroxypyrrolidin-3-yl]thiophene-2-carboxamide
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C22H20ClFN4O4S
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1
Kd = 9.787 nM
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CP0055903
 Compound Info 
5-Bromo-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-furamide
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C19H18BrN3O6
  1
1
Kd = 13.4 nM
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CP0042272
 Compound Info 
4-chloro-N-(1-(2-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenylamino)-2-oxoethyl)-1H-1,2,4-triazol-3-yl)cyclopenta-1,3-dienecarboxamide
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C20H14ClFN6O3S
  1
1
Kd = 13.67 nM
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CP0042273
 Compound Info 
5-Chloro-N-({(5S)-3-[4-(dimethylamino)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide
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C17H18ClN3O3S
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1
Kd = 13.9 nM
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CP0055886
 Compound Info 
(R)-4-chloro-N-(1-(2-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenylamino)-2-oxoethyl)pyrrolidin-3-yl)cyclopenta-1,3-dienecarboxamide
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C22H20ClFN4O3S
  1
1
Kd = 14.03 nM
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CP0881608
 Compound Info 
5-chloro-N-[(1R,2S,4R)-4-[[2-fluoro-4-(2-oxopyridin-1-yl)phenyl]carbamoyl]-2-methoxycyclopentyl]thiophene-2-carboxamide
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C23H21ClFN3O4S
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1
Kd = 14.5 nM
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CP0055902
 Compound Info 
4-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl}benzamide
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C21H20ClN3O5
  1
1
Kd = 15 nM
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CP0086067
 Compound Info 
BAY 59-7939 Analog 15
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C20H22ClN3O4S
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1
Kd = 15.3 nM
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CP0861233
 Compound Info 
(3S,4S)-3-[[(5-chlorothiophene-2-carbonyl)amino]methyl]-N-[2-fluoro-4-(2-oxopyridin-1-yl)phenyl]-4-methoxypyrrolidine-1-carboxamide
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C23H22ClFN4O4S
  1
1
Kd = 16.3 nM
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CP0091646
 Compound Info 
(2R,3R)-2-(3-Carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)-benzoylamino]-butyric acid methyl ester
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C25H26N4O4
  1
1
Kd = 16.84 nM
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CP0658242
 Compound Info 
5-chloro-N-[3-oxo-3-[4-(3-oxomorpholin-4-yl)anilino]propyl]thiophene-2-carboxamide
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C18H18ClN3O4S
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1
Kd = 24.35 nM
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CP0675735
 Compound Info 
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-2-[(1-cyclopropylpiperidin-4-yl)carbamoyl]benzimidazole-5-carboxylic acid
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C25H24ClN5O4S
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1
Kd = 27.03 nM
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CP0056149
 Compound Info 
BAY 59-7939 Analog 18
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C20H21N3O5S
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1
Kd = 29.95 nM
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CP0675784
 Compound Info 
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-5-(hydroxymethyl)-N-[4-(3-oxomorpholin-4-yl)phenyl]pyrazole-3-carboxamide
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C23H20ClN5O5S
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1
Kd = 33.43 nM
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CP0881606
 Compound Info 
5-chloro-N-[(3R,4S)-4-fluoro-1-[2-[2-fluoro-4-(2-oxopyridin-1-yl)anilino]-2-oxoethyl]pyrrolidin-3-yl]thiophene-2-carboxamide
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C22H19ClF2N4O3S
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1
Kd = 34.33 nM
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CP0675674
 Compound Info 
5-chloro-N-[3-oxo-3-[4-(3-oxomorpholin-4-yl)-3-(trifluoromethyl)anilino]propyl]thiophene-2-carboxamide
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C19H17ClF3N3O4S
  1
1
Kd = 42.4 nM
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CP0134238
 Compound Info 
1-[2-(4-bromoanilino)-2-oxoethyl]-N-(1-propan-2-ylpiperidin-4-yl)indole-2-carboxamide
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C25H29BrN4O2
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1
Kd = 44.5 nM
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CP0091694
 Compound Info 
BAY 59-7939 Analog 10
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C19H20ClFN4O3S
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1
Kd = 44.75 nM
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CP0657836
 Compound Info 
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-5-(2-methoxyethoxy)-N-(1-propan-2-ylpiperidin-4-yl)pyrrolo[2,3-c]pyridine-2-carboxamide
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C26H33ClN6O4
  1
1
Kd = 48.45 nM
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CP0675737
 Compound Info 
5-chloro-N-[2-[[4-(2-oxopyrazin-1-yl)phenyl]sulfamoyl]ethyl]thiophene-2-carboxamide
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C17H15ClN4O4S2
  1
1
Kd = 55.17 nM
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CP0265488
 Compound Info 
N-[(3S)-1-(4,7-diazabicyclo[4.3.0]nona-2,4,8,10-tetraen-8-ylmethyl)-2-oxo-pyrrolidin-3-yl]-7-thia-2-azabicyclo[4.3.0]nona-2,4,8,10-tetraene-8-sulfonamide
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C19H17N5O3S2
  1
1
Kd = 83.1 nM
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CP0038193
 Compound Info 
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
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C21H19N5O3S2
  1
1
Kd = 106.77 nM
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CP0683686
 Compound Info 
N-[(3S)-1-[(2-amino-3H-benzimidazol-5-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
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C23H23N5O4S
  1
1
Kd = 115.5 nM
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CP0772413
 Compound Info 
N-[[2-(2-amino-2-oxoethoxy)-4-carbamimidoylphenyl]methyl]-2-[2,6-difluoro-4-(pyridin-2-ylmethoxy)phenyl]-2-ethoxyacetamide;hydrochloride
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C26H28ClF2N5O5
  1
1
Kd = 116.53 nM
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CP0042254
 Compound Info 
1-[(3-carbamimidoylphenyl)methyl]-N-[(3,5-dimethylphenyl)methyl]-4-methyl-1H-indole-2-carboxamide
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C27H28N4O
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1
Kd = 120.33 nM
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CP0683616
 Compound Info 
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[4-(2-oxopyrazin-1-yl)phenyl]benzimidazole-2-carboxamide
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C25H18ClN7O3
  1
1
Kd = 152 nM
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CP0106638
 Compound Info 
5-Chloro-N-({(5R)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-sulfonamide
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C18H18ClN3O6S2
  1
1
Kd = 177.95 nM
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CP0247833
 Compound Info 
5-Chloro-N-{[(5S)-3-(3-fluoro-4-thiomorpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}thiophene-2-carboxamide
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C19H19ClFN3O3S2
  1
1
Kd = 179 nM
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CP0055397
 Compound Info 
6-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)nicotinamide
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C20H19ClN4O5
  1
1
Kd = 182.5 nM
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CP0106631
 Compound Info 
2-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)-1,3-thiazole-5-carboxamide
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C18H17ClN4O5S
  1
1
Kd = 191.5 nM
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CP0036404
 Compound Info 
4-({4-[(6-CHLORO-1-BENZOTHIEN-2-YL)SULFONYL]-2-OXOPIPERAZIN-1-YL}METHYL)BENZENECARBOXIMIDAMIDE
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C20H19ClN4O3S2
  1
1
Kd = 265 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0658457
 Compound Info 
(2R)-2-(4-carbamimidoylanilino)-2-[5-ethoxy-2-fluoro-3-(1-methylpiperidin-4-yl)oxyphenyl]acetic acid
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C23H29FN4O4
  1
1
Kd = 284 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0055901
 Compound Info 
3-[2-Oxo-3-(S)-(5-pyridin-4-ylthiophene-2-ylsulfonylamino)-pyrrolidin-1-ylmethyl]benzamidine
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C21H21N5O3S2
  1
1
Kd = 299 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0071439
 Compound Info 
5-Chloro-N-{[(5S)-3-(3-fluoro-4-pyrrolidin-1-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}thiophene-2-carboxamide
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C19H19ClFN3O3S
  1
1
Kd = 309 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0091693
 Compound Info 
BAY 59-7939 Analog 11
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C19H18ClN3O4S
  14
1 IC50 = 0.542 nM
2 IC50 = 0.547 nM
3 IC50 = 0.556 nM
4 IC50 = 0.581 nM
5 IC50 = 0.588 nM
6 IC50 = 0.633 nM
7 IC50 = 0.634 nM
8 IC50 = 0.691 nM
9 IC50 = 0.699 nM
10 IC50 = 0.725 nM
11 IC50 = 0.738 nM
12 IC50 = 0.762 nM
13 IC50 = 4 nM
14 Kd = 1.985 nM
CP0091646
 Compound Info 
(2R,3R)-2-(3-Carbamimidoyl-benzyl)-3-[4-(1-oxy-pyridin-4-yl)-benzoylamino]-butyric acid methyl ester
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C25H26N4O4
  15
1 IC50 = 0.586 nM
2 IC50 = 0.623 nM
3 IC50 = 0.682 nM
4 IC50 = 0.702 nM
5 IC50 = 0.734 nM
6 IC50 = 0.747 nM
7 IC50 = 0.784 nM
8 IC50 = 0.823 nM
9 IC50 = 0.851 nM
10 IC50 = 0.865 nM
11 IC50 = 0.929 nM
12 IC50 = 0.933 nM
13 Kd = 89.31 nM
14 Ki = 0.4 nM
15 Ki = 0.5 nM
CP0658153
 Compound Info 
3-[[(5-chlorothiophene-2-carbonyl)amino]methyl]-N-[2-fluoro-4-(2-oxopyridin-1-yl)phenyl]-1,2,4-oxadiazole-5-carboxamide
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C20H13ClFN5O4S
  13
1 IC50 = 0.64 nM
2 IC50 = 0.667 nM
3 IC50 = 0.674 nM
4 IC50 = 0.708 nM
5 IC50 = 0.723 nM
6 IC50 = 0.757 nM
7 IC50 = 0.774 nM
8 IC50 = 0.796 nM
9 IC50 = 0.816 nM
10 IC50 = 0.819 nM
11 IC50 = 0.856 nM
12 IC50 = 0.891 nM
13 Kd = 1.88 nM
CP0055905
 Compound Info 
BAY 59-7939 Analog 14
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C19H19ClN4O5S
  14
1 IC50 = 0.658 nM
2 IC50 = 0.676 nM
3 IC50 = 0.737 nM
4 IC50 = 0.742 nM
5 IC50 = 0.765 nM
6 IC50 = 0.787 nM
7 IC50 = 0.803 nM
8 IC50 = 0.808 nM
9 IC50 = 0.824 nM
10 IC50 = 0.839 nM
11 IC50 = 0.854 nM
12 IC50 = 0.863 nM
13 IC50 = 2.5 nM
14 Kd = 2.3 nM
CP0056149
 Compound Info 
BAY 59-7939 Analog 18
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C20H21N3O5S
  14
1 IC50 = 0.684 nM
2 IC50 = 0.707 nM
3 IC50 = 0.779 nM
4 IC50 = 0.787 nM
5 IC50 = 0.993 nM
6 IC50 = 1.02 nM
7 IC50 = 1.03 nM
8 IC50 = 1.05 nM
9 IC50 = 1.06 nM
10 IC50 = 1.14 nM
11 IC50 = 1.15 nM
12 IC50 = 1.2 nM
13 IC50 = 4.2 nM
14 Kd = 3.72 nM
CP0649829
 Compound Info 
5-chloro-N-[1-[2-[2-fluoro-4-(2-oxopyridin-1-yl)anilino]-2-oxoethyl]-4-methoxypyrrolidin-3-yl]thiophene-2-carboxamide
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C23H22ClFN4O4S
  9
1 IC50 = 0.976 nM
2 IC50 = 1.03 nM
3 IC50 = 1.04 nM
4 IC50 = 1.06 nM
5 IC50 = 1.1 nM
6 IC50 = 1.14 nM
7 IC50 = 1.15 nM
8 IC50 = 1.16 nM
9 IC50 = 1.21 nM
CP0071439
 Compound Info 
5-Chloro-N-{[(5S)-3-(3-fluoro-4-pyrrolidin-1-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}thiophene-2-carboxamide
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C19H19ClFN3O3S
  14
1 IC50 = 1.11 nM
2 IC50 = 1.58 nM
3 IC50 = 1.62 nM
4 IC50 = 1.66 nM
5 IC50 = 1.72 nM
6 IC50 = 2.01 nM
7 IC50 = 2.03 nM
8 IC50 = 2.06 nM
9 IC50 = 2.12 nM
10 IC50 = 2.18 nM
11 IC50 = 2.28 nM
12 IC50 = 2.32 nM
13 IC50 = 40 nM
14 Kd = 7.76 nM
CP0675784
 Compound Info 
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-5-(hydroxymethyl)-N-[4-(3-oxomorpholin-4-yl)phenyl]pyrazole-3-carboxamide
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C23H20ClN5O5S
  12
1 IC50 = 1.13 nM
2 IC50 = 1.22 nM
3 IC50 = 1.24 nM
4 IC50 = 1.39 nM
5 IC50 = 1.4 nM
6 IC50 = 1.58 nM
7 IC50 = 1.59 nM
8 IC50 = 1.61 nM
9 IC50 = 1.64 nM
10 IC50 = 1.8 nM
11 IC50 = 1.83 nM
12 Kd = 37.4 nM
CP0042272
 Compound Info 
4-chloro-N-(1-(2-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenylamino)-2-oxoethyl)-1H-1,2,4-triazol-3-yl)cyclopenta-1,3-dienecarboxamide
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C20H14ClFN6O3S
  14
1 IC50 = 1.19 nM
2 IC50 = 1.25 nM
3 IC50 = 1.26 nM
4 IC50 = 1.28 nM
5 IC50 = 1.35 nM
6 IC50 = 1.41 nM
7 IC50 = 1.46 nM
8 IC50 = 1.53 nM
9 IC50 = 1.55 nM
10 IC50 = 1.66 nM
11 IC50 = 1.72 nM
12 IC50 = 1.73 nM
13 Kd = 5.855 nM
14 Ki = 6 nM
CP0036404
 Compound Info 
4-({4-[(6-CHLORO-1-BENZOTHIEN-2-YL)SULFONYL]-2-OXOPIPERAZIN-1-YL}METHYL)BENZENECARBOXIMIDAMIDE
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C20H19ClN4O3S2
  15
1 IC50 = 1.23 nM
2 IC50 = 1.45 nM
3 IC50 = 1.51 nM
4 IC50 = 1.53 nM
5 IC50 = 1.54 nM
6 IC50 = 1.61 nM
7 IC50 = 1.64 nM
8 IC50 = 1.69 nM
9 IC50 = 1.74 nM
10 IC50 = 1.83 nM
11 IC50 = 1.91 nM
12 IC50 = 1.92 nM
13 Kd = 2.281 nM
14 Ki = 1 nM
15 Ki = 1.3 nM
CP0055886
 Compound Info 
(R)-4-chloro-N-(1-(2-(2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenylamino)-2-oxoethyl)pyrrolidin-3-yl)cyclopenta-1,3-dienecarboxamide
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C22H20ClFN4O3S
  13
1 IC50 = 1.67 nM
2 IC50 = 1.73 nM
3 IC50 = 1.75 nM
4 IC50 = 1.76 nM
5 IC50 = 1.83 nM
6 IC50 = 1.85 nM
7 IC50 = 1.89 nM
8 IC50 = 1.9 nM
9 IC50 = 1.98 nM
10 IC50 = 2.04 nM
11 IC50 = 2.05 nM
12 IC50 = 2.07 nM
13 Ki = 8 nM
CP0134238
 Compound Info 
1-[2-(4-bromoanilino)-2-oxoethyl]-N-(1-propan-2-ylpiperidin-4-yl)indole-2-carboxamide
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C25H29BrN4O2
  14
1 IC50 = 1.71 nM
2 IC50 = 1.8 nM
3 IC50 = 2.03 nM
4 IC50 = 2.11 nM
5 IC50 = 2.17 nM
6 IC50 = 2.39 nM
7 IC50 = 2.4 nM
8 IC50 = 2.65 nM
9 IC50 = 2.66 nM
10 IC50 = 2.81 nM
11 IC50 = 2.87 nM
12 IC50 = 2.96 nM
13 Kd = 2.014 nM
14 Ki = 3 nM
CP0675674
 Compound Info 
5-chloro-N-[3-oxo-3-[4-(3-oxomorpholin-4-yl)-3-(trifluoromethyl)anilino]propyl]thiophene-2-carboxamide
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C19H17ClF3N3O4S
  13
1 IC50 = 1.9 nM
2 IC50 = 1.91 nM
3 IC50 = 2.01 nM
4 IC50 = 2.55 nM
5 IC50 = 2.62 nM
6 IC50 = 3.11 nM
7 IC50 = 3.38 nM
8 IC50 = 3.4 nM
9 IC50 = 3.63 nM
10 IC50 = 3.71 nM
11 IC50 = 3.93 nM
12 IC50 = 4.57 nM
13 Kd = 13.07 nM
CP0657836
 Compound Info 
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-5-(2-methoxyethoxy)-N-(1-propan-2-ylpiperidin-4-yl)pyrrolo[2,3-c]pyridine-2-carboxamide
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C26H33ClN6O4
  12
1 IC50 = 2.76 nM
2 IC50 = 3.34 nM
3 IC50 = 3.65 nM
4 IC50 = 4.81 nM
5 IC50 = 5.13 nM
6 IC50 = 5.19 nM
7 IC50 = 5.2 nM
8 IC50 = 5.23 nM
9 IC50 = 5.62 nM
10 IC50 = 5.9 nM
11 IC50 = 6.49 nM
12 Kd = 18.54 nM
CP0055903
 Compound Info 
5-Bromo-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-furamide
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C19H18BrN3O6
  14
1 IC50 = 2.88 nM
2 IC50 = 3.61 nM
3 IC50 = 3.67 nM
4 IC50 = 3.89 nM
5 IC50 = 3.96 nM
6 IC50 = 4.08 nM
7 IC50 = 4.18 nM
8 IC50 = 4.21 nM
9 IC50 = 4.29 nM
10 IC50 = 4.52 nM
11 IC50 = 4.76 nM
12 IC50 = 4.99 nM
13 IC50 = 26 nM
14 Kd = 18.4 nM
CP0042273
 Compound Info 
5-Chloro-N-({(5S)-3-[4-(dimethylamino)phenyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide
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C17H18ClN3O3S
  14
1 IC50 = 3.15 nM
2 IC50 = 3.88 nM
3 IC50 = 4.35 nM
4 IC50 = 4.39 nM
5 IC50 = 4.68 nM
6 IC50 = 4.97 nM
7 IC50 = 5.1 nM
8 IC50 = 5.86 nM
9 IC50 = 5.87 nM
10 IC50 = 5.96 nM
11 IC50 = 6.15 nM
12 IC50 = 6.75 nM
13 IC50 = 74 nM
14 Kd = 15.61 nM
CP0055902
 Compound Info 
4-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl]methyl}benzamide
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C21H20ClN3O5
  13
1 IC50 = 3.58 nM
2 IC50 = 4.07 nM
3 IC50 = 4.27 nM
4 IC50 = 4.38 nM
5 IC50 = 4.43 nM
6 IC50 = 4.55 nM
7 IC50 = 4.59 nM
8 IC50 = 4.6 nM
9 IC50 = 4.77 nM
10 IC50 = 4.92 nM
11 IC50 = 5.47 nM
12 IC50 = 20 nM
13 Kd = 20.9 nM
CP0658242
 Compound Info 
5-chloro-N-[3-oxo-3-[4-(3-oxomorpholin-4-yl)anilino]propyl]thiophene-2-carboxamide
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C18H18ClN3O4S
  13
1 IC50 = 5.64 nM
2 IC50 = 5.75 nM
3 IC50 = 6.55 nM
4 IC50 = 7.29 nM
5 IC50 = 7.55 nM
6 IC50 = 7.92 nM
7 IC50 = 7.98 nM
8 IC50 = 8.29 nM
9 IC50 = 8.69 nM
10 IC50 = 9.14 nM
11 IC50 = 9.68 nM
12 IC50 = 9.74 nM
13 Kd = 130.65 nM
CP0683616
 Compound Info 
1-[2-[(5-chloropyridin-2-yl)amino]-2-oxoethyl]-N-[4-(2-oxopyrazin-1-yl)phenyl]benzimidazole-2-carboxamide
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C25H18ClN7O3
  13
1 IC50 = 8.98 nM
2 IC50 = 10.6 nM
3 IC50 = 11.6 nM
4 IC50 = 11.9 nM
5 IC50 = 12 nM
6 IC50 = 12.7 nM
7 IC50 = 13.3 nM
8 IC50 = 13.4 nM
9 IC50 = 13.9 nM
10 IC50 = 14.1 nM
11 IC50 = 16.7 nM
12 IC50 = 17.2 nM
13 Kd = 77.49 nM
CP0247833
 Compound Info 
5-Chloro-N-{[(5S)-3-(3-fluoro-4-thiomorpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}thiophene-2-carboxamide
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C19H19ClFN3O3S2
  13
1 IC50 = 12.9 nM
2 IC50 = 13.5 nM
3 IC50 = 13.7 nM
4 IC50 = 14.7 nM
5 IC50 = 15 nM
6 IC50 = 15.2 nM
7 IC50 = 16.1 nM
8 IC50 = 17.2 nM
9 IC50 = 17.4 nM
10 IC50 = 17.7 nM
11 IC50 = 17.9 nM
12 IC50 = 90 nM
13 Kd = 33.12 nM
CP0772413
 Compound Info 
N-[[2-(2-amino-2-oxoethoxy)-4-carbamimidoylphenyl]methyl]-2-[2,6-difluoro-4-(pyridin-2-ylmethoxy)phenyl]-2-ethoxyacetamide;hydrochloride
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C26H28ClF2N5O5
  12
1 IC50 = 15.2 nM
2 IC50 = 20.3 nM
3 IC50 = 22.5 nM
4 IC50 = 22.7 nM
5 IC50 = 22.8 nM
6 IC50 = 23 nM
7 IC50 = 23.6 nM
8 IC50 = 31.6 nM
9 IC50 = 33.4 nM
10 IC50 = 38.6 nM
11 IC50 = 38.9 nM
12 Kd = 37.2 nM
CP0038193
 Compound Info 
N-[(3S)-1-[(1-aminoisoquinolin-7-yl)methyl]-2-oxopyrrolidin-3-yl]thieno[3,2-b]pyridine-2-sulfonamide
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C21H19N5O3S2
  14
1 IC50 = 17.6 nM
2 IC50 = 27.1 nM
3 IC50 = 31.5 nM
4 IC50 = 32 nM
5 IC50 = 32.4 nM
6 IC50 = 37 nM
7 IC50 = 37.4 nM
8 IC50 = 37.7 nM
9 IC50 = 42.1 nM
10 IC50 = 42.7 nM
11 IC50 = 42.9 nM
12 IC50 = 43.7 nM
13 Kd = 85.35 nM
14 Ki = 22 nM
CP0675735
 Compound Info 
1-[[5-(5-chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-2-[(1-cyclopropylpiperidin-4-yl)carbamoyl]benzimidazole-5-carboxylic acid
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C25H24ClN5O4S
  12
1 IC50 = 18.1 nM
2 IC50 = 18.3 nM
3 IC50 = 19.2 nM
4 IC50 = 19.7 nM
5 IC50 = 19.8 nM
6 IC50 = 20.4 nM
7 IC50 = 21 nM
8 IC50 = 21.4 nM
9 IC50 = 21.6 nM
10 IC50 = 23.8 nM
11 IC50 = 24.8 nM
12 Kd = 34.21 nM
CP0265488
 Compound Info 
N-[(3S)-1-(4,7-diazabicyclo[4.3.0]nona-2,4,8,10-tetraen-8-ylmethyl)-2-oxo-pyrrolidin-3-yl]-7-thia-2-azabicyclo[4.3.0]nona-2,4,8,10-tetraene-8-sulfonamide
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C19H17N5O3S2
  12
1 IC50 = 19.3 nM
2 IC50 = 20.3 nM
3 IC50 = 20.5 nM
4 IC50 = 21.8 nM
5 IC50 = 22.9 nM
6 IC50 = 25.5 nM
7 IC50 = 25.9 nM
8 IC50 = 27.4 nM
9 IC50 = 27.6 nM
10 IC50 = 27.8 nM
11 IC50 = 31.2 nM
12 Kd = 4.938 nM
CP0091694
 Compound Info 
BAY 59-7939 Analog 10
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C19H20ClFN4O3S
  14
1 IC50 = 24.6 nM
2 IC50 = 25.8 nM
3 IC50 = 28.1 nM
4 IC50 = 30.1 nM
5 IC50 = 32.8 nM
6 IC50 = 33.8 nM
7 IC50 = 34.1 nM
8 IC50 = 34.7 nM
9 IC50 = 36.9 nM
10 IC50 = 37.9 nM
11 IC50 = 38.1 nM
12 IC50 = 40.3 nM
13 IC50 = 140 nM
14 Kd = 45.75 nM
CP0675737
 Compound Info 
5-chloro-N-[2-[[4-(2-oxopyrazin-1-yl)phenyl]sulfamoyl]ethyl]thiophene-2-carboxamide
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C17H15ClN4O4S2
  11
1 IC50 = 26.7 nM
2 IC50 = 29.7 nM
3 IC50 = 29.9 nM
4 IC50 = 30 nM
5 IC50 = 31.2 nM
6 IC50 = 32.2 nM
7 IC50 = 32.9 nM
8 IC50 = 34.2 nM
9 IC50 = 38.5 nM
10 IC50 = 47.5 nM
11 Kd = 37.93 nM
CP0055901
 Compound Info 
3-[2-Oxo-3-(S)-(5-pyridin-4-ylthiophene-2-ylsulfonylamino)-pyrrolidin-1-ylmethyl]benzamidine
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C21H21N5O3S2
  14
1 IC50 = 40.8 nM
2 IC50 = 42.9 nM
3 IC50 = 46.1 nM
4 IC50 = 46.5 nM
5 IC50 = 49.4 nM
6 IC50 = 49.8 nM
7 IC50 = 50.1 nM
8 IC50 = 53.5 nM
9 IC50 = 58.5 nM
10 IC50 = 60.8 nM
11 IC50 = 61.8 nM
12 IC50 = 63.9 nM
13 Kd = 192.45 nM
14 Ki = 55 nM
CP0055397
 Compound Info 
6-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)nicotinamide
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C20H19ClN4O5
  14
1 IC50 = 55.7 nM
2 IC50 = 63.6 nM
3 IC50 = 73.4 nM
4 IC50 = 74.3 nM
5 IC50 = 74.6 nM
6 IC50 = 75.8 nM
7 IC50 = 77.4 nM
8 IC50 = 83.4 nM
9 IC50 = 87 nM
10 IC50 = 87.5 nM
11 IC50 = 90.5 nM
12 IC50 = 94 nM
13 IC50 = 96.1 nM
14 Kd = 53.94 nM
CP0042254
 Compound Info 
1-[(3-carbamimidoylphenyl)methyl]-N-[(3,5-dimethylphenyl)methyl]-4-methyl-1H-indole-2-carboxamide
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C27H28N4O
  13
1 IC50 = 57 nM
2 IC50 = 57.3 nM
3 IC50 = 64.5 nM
4 IC50 = 67.7 nM
5 IC50 = 68.4 nM
6 IC50 = 69.9 nM
7 IC50 = 72.5 nM
8 IC50 = 74.5 nM
9 IC50 = 76.3 nM
10 IC50 = 78.4 nM
11 IC50 = 81.2 nM
12 Kd = 23.05 nM
13 Ki = 9 nM
CP0086067
 Compound Info 
BAY 59-7939 Analog 15
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C20H22ClN3O4S
  13
1 IC50 = 57.8 nM
2 IC50 = 58.1 nM
3 IC50 = 68.7 nM
4 IC50 = 71.6 nM
5 IC50 = 75.7 nM
6 IC50 = 77.1 nM
7 IC50 = 88.6 nM
8 IC50 = 93.1 nM
9 IC50 = 108 nM
10 IC50 = 115 nM
11 IC50 = 116 nM
12 IC50 = 124 nM
13 IC50 = 1260 nM
CP0106631
 Compound Info 
2-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)-1,3-thiazole-5-carboxamide
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C18H17ClN4O5S
  11
1 IC50 = 105 nM
2 IC50 = 140 nM
3 IC50 = 152 nM
4 IC50 = 155 nM
5 IC50 = 160 nM
6 IC50 = 167 nM
7 IC50 = 173 nM
8 IC50 = 175 nM
9 IC50 = 186 nM
10 IC50 = 189 nM
11 IC50 = 290 nM
CP0106638
 Compound Info 
5-Chloro-N-({(5R)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-sulfonamide
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C18H18ClN3O6S2
  13
1 IC50 = 397 nM
2 IC50 = 411 nM
3 IC50 = 415 nM
4 IC50 = 425 nM
5 IC50 = 440 nM
6 IC50 = 449 nM
7 IC50 = 471 nM
8 IC50 = 483 nM
9 IC50 = 502 nM
10 IC50 = 508 nM
11 IC50 = 514 nM
12 IC50 = 517 nM
13 IC50 = 1200 nM
CP0658457
 Compound Info 
(2R)-2-(4-carbamimidoylanilino)-2-[5-ethoxy-2-fluoro-3-(1-methylpiperidin-4-yl)oxyphenyl]acetic acid
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C23H29FN4O4
  11
1 IC50 = 706 nM
2 IC50 = 736 nM
3 IC50 = 764 nM
4 IC50 = 901 nM
5 IC50 = 992 nM
6 IC50 = 1010 nM
7 IC50 = 1030 nM
8 IC50 = 1060 nM
9 IC50 = 1090 nM
10 IC50 = 1360 nM
11 IC50 = 1500 nM
CP0683686
 Compound Info 
N-[(3S)-1-[(2-amino-3H-benzimidazol-5-yl)methyl]-2-oxopyrrolidin-3-yl]-7-methoxynaphthalene-2-sulfonamide
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C23H23N5O4S
  11
1 IC50 = 3040 nM
2 IC50 = 3190 nM
3 IC50 = 3340 nM
4 IC50 = 3550 nM
5 IC50 = 3740 nM
6 IC50 = 3750 nM
7 IC50 = 3950 nM
8 IC50 = 4280 nM
9 IC50 = 5070 nM
10 IC50 = 7020 nM
11 Kd = 2387.5 nM
Clinical Information about the Protein
Target 1 ( Coagulation factor Xa (F10) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Thrombosis [ICD-11: DB61-GB90]
2 Venous thromboembolism [ICD-11: BD72]
3 Venous thrombosis [ICD-11: BA43]
4 Deep vein thrombosis [ICD-11: BD71]
5 Angina pectoris [ICD-11: BA40]
6 Acute myeloid leukaemia [ICD-11: 2A60]
7 Psoriasis vulgaris [ICD-11: EA90]
Approved Drug(s) 4 Approved Drugs  4
1 Apixaban
 Drug Info 
Approved
Thrombosis
2 BETRIXABAN
 Drug Info 
Approved
Venous thromboembolism
3 Fondaparinux sodium
 Drug Info 
Approved
Venous thrombosis
4 Rivaroxaban
 Drug Info 
Approved
Deep vein thrombosis
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 GW-813893
 Drug Info 
Phase 2
Thrombosis
2 LY-517717
 Drug Info 
Phase 2
Thrombosis
3 BIBT986
 Drug Info 
Phase 1
Thrombosis
Discontinued Drug(s) 8 Discontinued Drugs  8
1 Otamixaban
 Drug Info 
Discontinued in Phase 3
Angina pectoris
2 Valspodar
 Drug Info 
Discontinued in Phase 3
Acute myeloid leukaemia
3 Octopamine
 Drug Info 
Discontinued in Phase 2a
Thrombosis
4 PD-348292
 Drug Info 
Discontinued in Phase 2
Thrombosis
5 R-68151
 Drug Info 
Discontinued in Phase 2
Psoriasis vulgaris
6 TAK-442
 Drug Info 
Discontinued in Phase 2
Thrombosis
7 DPC 423
 Drug Info 
Discontinued in Phase 1
Thrombosis
8 EMD-503982
 Drug Info 
Discontinued in Phase 1
Thrombosis
Investigative Drug(s) 1 Investigative Drug  1
1 SN429
 Drug Info 
Investigative
Thrombosis