Therapeutic Targets Database
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TTD Target ID: TTDS00202

Target Information
NameThrombin    
Type of targetSuccessful target    
SynonymsCoagulation factor II    
Prothrombin    
DiseaseCoagulative disorders
[ICD9: 286   ICD10: D65-D69]
[1][2][3]
Coronary atherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[4]
Gliomas
[ICD9: 191   ICD10: C71]
[5]
Heparin-induced thrombocytopenia type II
[ICD9: 287.3, 287.4, 287.5   ICD10: D69.6, P61.0]
[6]
Multiple organ failure[7]
Thromboembolic disorders
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[8][9][10]
Thrombosis
[ICD9: 437.6, 453, 671.5, 671.9   ICD10: I80-I82]
[11][4][12]
Thrombotic disease[13][14][15]
Drug(s)ArgatrobanApprovedThrombosis[16][17][18]
BivalirudinApprovedThrombocytopenia[17]
DabigatranApprovedStroke prevention in atrial fibrillation[19]
LepirudinApprovedThrombocytopenia[6]
XimelagatranApprovedAnticoagulant[20]
XimelegatranMarketedAtrial fibrillation, venous thromboembolism, myocardial infarction[21]
SR-123781APhase III completed, and Positive results in a large European Phase III trialVenous Thromboembolism[22][23]
AZD0837Phase II completedNonvalvular Atrial Fibrillation, Thrombosis[24]
DermolastinPhase IIAtopic Dermatitis, Alpha 1 Antitrypsin Deficiency[25][26][27][28]
DermolastinHalted in Phase IChronic Obstructive Pulmonary Disease[25][26][27][28]
DermolastinHalted in Phase IEmphysema[25][26][27][28]
SR-123781ADiscontinued in Phase IIAcute Coronary Syndromes[22][23]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.21.5
PathwayComplement and coagulation cascades
Neuroactive ligand-receptor interaction
Regulation of actin cytoskeleton
UniProt IDP00734
PDB Structure1A2C; 1A3B; 1A3E; 1A46; 1A4W; 1A5G; 1A61; 1ABI; 1ABJ; 1AD8; 1AE8; 1AFE; 1AHT; 1AI8; 1AIX; 1AWF; 1AWH; 1AY6; 1B5G; 1B7X; 1BA8; 1BB0; 1BCU; 1BHX; 1BMM; 1BMN; 1BTH; 1C1U; 1C1V; 1C1W; 1C4U; 1C4V; 1C4Y; 1C5L; 1C5N; 1C5O; 1CA8; 1D3D; 1D3P; 1D3Q; 1D3T; 1D4P; 1D6W; 1D9I; 1DE7; 1DIT; 1DM4; 1DOJ; 1DWB; 1DWC; 1DWD; 1DWE; 1DX5; 1E0F; 1EB1; 1EOJ; 1EOL; 1FPC; 1FPH; 1G30; 1G32; 1G37; 1GHV; 1GHW; 1GHX; 1GHY; 1GJ4; 1GJ5; 1H8D; 1H8I; 1HAG; 1HAH; 1HAI; 1HAO; 1HAP; 1HBT; 1HDT; 1HGT; 1HLT; 1HUT; 1HXE; 1HXF; 1IHS; 1IHT; 1JMO; 1JOU; 1JWT; 1K21; 1K22; 1KTS; 1KTT; 1LHC; 1LHD; 1LHE; 1LHF; 1LHG; 1MH0; 1MU6; 1MU8; 1MUE; 1NM6; 1NO9; 1NRN; 1NRO; 1NRP; 1NRQ; 1NRR; 1NRS; 1NT1; 1NU7; 1NU9; 1NY2; 1NZQ; 1O0D; 1O2G; 1O5G; 1OOK; 1OYT; 1P8V; 1PPB; 1QBV; 1QHR; 1QJ1; 1QJ6; 1QJ7; 1QUR; 1RD3; 1RIW; 1SB1; 1SFQ; 1SG8; 1SGI; 1SHH; 1SL3; 1SR5; 1T4U; 1T4V; 1TA2; 1TA6; 1TB6; 1TBZ; 1THP; 1THR; 1THS; 1TMB; 1TMT; 1TMU; 1TOM; 1TQ0; 1TQ7; 1TWX; 1UMA; 1UVS; 1VR1; 1VZQ; 1W7G; 1WAY; 1WBG; 1XM1; 1XMN; 1YPE; 1YPG; 1YPJ; 1YPK; 1YPL; 1YPM; 1Z71; 1Z8I; 1Z8J; 1ZGI; 1ZGV; 1ZRB; 2A0Q; 2A2X; 2A45; 2AFQ; 2ANK; 2ANM; 2B5T; 2BDY; 2BVR; 2BVS; 2BVX; 2BXT; 2BXU; 2C8W; 2C8X; 2C8Y; 2C8Z; 2C90; 2C93; 2CF8; 2CF9; 2CN0; 2FEQ; 2FES; 2GDE; 2GP9; 2H9T; 2HGT; 2HNT; 2HPP; 2HPQ; 2HWL; 2JH0; 2JH5; 2JH6; 2OD3; 2PGB; 2PGQ; 2PKS; 2PW8; 2R2M; 2THF; 2UUF; 2UUJ; 2UUK; 2V3H; 2V3O; 2ZC9; 2ZDA; 2ZDV; 2ZF0; 2ZFF; 2ZFP; 2ZFQ; 2ZFR; 2ZG0; 2ZGB; 2ZGX; 2ZHE; 2ZHF; 2ZHQ; 2ZHW; 2ZI2; 2ZIQ; 2ZNK; 2ZO3; 3B23; 3B9F; 3BEF; 3BEI; 3BF6; 3BIU; 3BIV; 3BV9; 3C1K; 3C27; 3D49; 3DA9; 3DD2; 3DHK; 3DT0; 3DUX; 3E6P; 3EE0; 3EGK; 3EQ0; 3F68; 3GIC; 3GIS; 3HAT; 3HKJ; 3HTC; 3JZ1; 3JZ2; 3K65; 3LDX; 3LU9; 3NXP; 3P17; 3P6Z; 3P70; 3PMH; 3PO1; 3QDZ; 3QGN; 3QLP; 3QTO; 3QTV; 3QWC; 3QX5; 3R3G; 3RLW; 3RLY; 3RM0; 3RM2; 3RML; 3RMM; 3RMN; 3RMO; 3S7H; 3S7K; 3SHA; 3SHC; 3SI3; 3SI4; 3SQE; 3SQH; 3SV2; 3T5F; 3TU7; 3U69; 3U8O; 3U8R; 3U8T; 3U98; 3U9A; 3UTU; 3UWJ; 4AX9; 4AYV; 4AYY; 4AZ2; 4BAH; 4BAK; 4BAM; 4BAN; 4BAO; 4BAQ; 4DIH; 4DII; 4DT7; 4DY7; 4E05; 4E06; 4E7R; 4H6S; 4H6T; 4HFP; 4HFY; 4HTC; 4THN; 5GDS; 7KME; 8KME.    
FunctionThrombin, which cleaves bonds after arg and lys, converts fibrinogen to fibrin and activates factors v, vii, viii, xiii, and, in complex with thrombomodulin, protein c.    
SequenceMAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLEREC VEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHV NITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQE CSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASA QAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETG DGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYI DGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTEN DLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHP VCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDST RIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKY GFYTHVFRLKKWIQKVIDQFGE
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6,245,763
6,326,386
6,326,492
6,350,745
6,350,764
6,362,190
6,387,911
6,391,901
6,407,067
6,410,536
6,433,186
6,441,008
6,455,532
6,462,021
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6,586,418
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6,602,871
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6,635,651
6,642,253
6,670,381
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3,4-dichlorophenyl)[29]
(3-nitro-1H-pyrazol-1-yl)[29]
(3-nitro-1H-pyrazol-1-yl)[29]
(4-bromo-1H-pyrazol-1-yl)[29]
(4-nitro-1H-pyrazol-1-yl)[29]
(4-nitro-1H-pyrazol-1-yl)[29]
1- (HYDROXYMETHYLENEAMINO)-8-HYDROXY-OCTANE[30]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide[29]
2- (2-Hydroxy-phenyl)-1H-indole-5-carboxamidine[31]
2-NAPHTHALENESULFONIC ACID[30]
2-nas-phe (3-am)-4-[32]
3- (4-HYDROXY-PHENYL)PYRUVIC ACID[30]
3-chlorophenyl 2-oxo-2H-chromene-3-carboxylate[33]
4- (2,5-DIAMINO-5-HYDROXY-PENTYL)-PHENOL[30]
4- (3,4-Diethoxy-benzylamino)-benzamidine[34]
4- (4-Benzyloxy-3-methoxy-benzylamino)-benzamidine[34]
4-Iodobenzo[B]Thiophene-2-Carboxamidine[30]
4-TERT-BUTYLBENZENESULFONIC ACID[30]
4-[3- (4-CHLOROPHENYL)-1H-PYRAZOL-5-YL]PIPERIDINE[30]
5-desgalloylstachyurin[35]
6- (2-HYDROXY-CYCLOPENTYL)-7-OXO-HEPTANAMIDINE[30]
AC- (D)PHE-PRO-BOROHOMOLYS-OH[30]
AC- (D)PHE-PRO-BOROHOMOORNITHINE-OH[30]
AC- (D)PHE-PRO-BOROLYS-OH[30]
AZD0837[24]
Argatroban[16][17][18]
BCH-2763[9]
BENZOTHIAZOLE[30]
BIBR 1048[2]
BMS-344577[36]
BMS-740808[37]
Bbs-Arg- (D-Pip)-Gly-[38]
Bbs-Arg- (D-Pip)-Gly-[38]
Bbs-Arg- (D-Pip)-Gly-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Bbs-Arg- (D-Pip)-Gly-S-[38]
Beta- (2-Naphthyl)-Alanine[30]
Bivalirudin[17]
Bivalirudine[39]
CASUARIIN[35]
CHLORODYSINOSIN A[40]
COCHINCHINENENE B[41]
COCHINCHINENIN B[41]
CRA_8696[30]
D-Pro-Phe-Arg chloromethyl ketone[42]
D-leucyl-N- (3-chlorobenzyl)-L-prolinamide[30]
D-leucyl-N- (4-carbamimidoylbenzyl)-L-prolinamide[30]
D-phenylalanyl-N- (3-chlorobenzyl)-L-prolinamide[30]
D-phenylalanyl-N- (3-fluorobenzyl)-L-prolinamide[30]
D-phenylalanyl-N- (3-methylbenzyl)-L-prolinamide[30]
D-phenylalanyl-N-benzyl-L-prolinamide[30]
DYSINOSIN A[40]
Dabigatran[19]
Dermolastin[25][26][27][28]
Desirudine[39]
DuP 714[8]
DuP-714[43]
Efegatran[8]
Enoxaprin[44]
GR-133686[45]
Gamma-Carboxy-Glutamic Acid[46]
H376/95[17]
Hemi-Babim[30]
Heparin-Cantithrombin III[4]
Hirudin[1][17][11]
Hirulog[11]
Hirulog[47]
INOGATRAN[48]
L-370,518[11]
L-374,087[49]
L-375378[50]
LB30057[13]
LB30812[12]
Lepirudin[6]
Lepirudine[39]
Licostinel[51]
Lysophosphotidylserine[46]
MELAGATRAN[52]
METHYL-PHE-PRO-AMINO-CYCLOHEXYLGLYCINE[30]
Melagatran dipeptide[53]
Melogatran[4]
N4- (N,N-DIPHENYLCARBAMOYL)-AMINOGUANIDINE[30]
OSCILLARIN[40]
PEDUNCULAGIN[35]
PPACK[8]
RAZAXABAN[54]
RAZAXABAN HYDROCHLORIDE[55]
RWJ-50353[56]
RWJ-671818[57]
S-2238[58]
SC-79407[49]
SR-123781A[22][23]
Ximelagatran[20]
Ximelegatran[21]
beta-phenyl-D-phenylalanyl-N-propyl-L-prolinamide[30]
cyclotheonamide E[59]
cyclotheonamide E4[59]
cyclotheonamide E5[59]
macrocyclic tripeptide motif[60]
methyl L-phenylalaninate[30]
penta-O-galloyl-beta-glucoside[35]
tellimagrandin II[35]
CofactorVitamin K[61]
MultitargetDermolastin[25][26][27][28]
SR-123781A[22][23]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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National University of Singapore, Singapore


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