Details of the Target

General Information of Target

Target ID LDTP02208
Target Name Serine protease 1 (PRSS1)
Gene Name PRSS1
Gene ID 5644
Synonyms
TRP1; TRY1; TRYP1; Serine protease 1; EC 3.4.21.4; Anionic trypsin I; Anionic trypsin-I; Beta-trypsin; Cationic trypsinogen; Pretrypsinogen I; Trypsin I; Trypsin-1) [Cleaved into: Alpha-trypsin chain 1; Alpha-trypsin chain 2]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MNPLLILTFVAAALAAPFDDDDKIVGGYNCEENSVPYQVSLNSGYHFCGGSLINEQWVVS
AGHCYKSRIQVRLGEHNIEVLEGNEQFINAAKIIRHPQYDRKTLNNDIMLIKLSSRAVIN
ARVSTISLPTAPPATGTKCLISGWGNTASSGADYPDELQCLDAPVLSQAKCEASYPGKIT
SNMFCVGFLEGGKDSCQGDSGGPVVCNGQLQGVVSWGDGCAQKNKPGVYTKVYNYVKWIK
NTIAANS
Target Type
Successful
Target Bioclass
Enzyme
Family
Peptidase S1 family
Subcellular location
Secreted, extracellular space
Function
Has activity against the synthetic substrates Boc-Phe-Ser-Arg-Mec, Boc-Leu-Thr-Arg-Mec, Boc-Gln-Ala-Arg-Mec and Boc-Val-Pro-Arg-Mec. The single-chain form is more active than the two-chain form against all of these substrates.
TTD ID
T27602
Uniprot ID
P07477
DrugMap ID
TT2WR1T
Ensemble ID
ENST00000311737.12
HGNC ID
HGNC:9475
ChEMBL ID
CHEMBL209

Probe(s) Labeling This Target

PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DA-2
 Probe Info  		N.A.  LDD0072  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aprotinin Small molecular drug DB06692
Bortezomib Small molecular drug D0SH3I
Phase 3
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Melagatran Small molecular drug D01MUU
Ulinastatin Small molecular drug D0DF1R
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alpha-1 Antitrypsin . D04TEF
Investigative
Click To Hide/Show 128 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,3-di-p-tolyl-[1,3]Diazetidine-2,4-dione Small molecular drug D05ICF
1,3-dibenzyl-[1,3]Diazetidine-2,4-dione Small molecular drug D0F2YC
1-(3-amino-benzyl)-1h-indole-5-carboxamidine Small molecular drug D09TNA
1-(3-nitro-benzyl)-1h-indole-5-carboxamidine Small molecular drug D0EH1F
1-benzyl-1h-indole-5-carboxamidine Small molecular drug D0M2PE
2-(2-hydroxy-phenyl)-1h-indole-5-carboxamidine Small molecular drug D08OLP
2-(2-hydroxy-phenyl)-1h-indole-5-carboxamidine Small molecular drug DB02463
2-(2-iodo-phenyl)-benzo[D][1,3]Oxazin-4-one Small molecular drug D0J2SM
2-naphthalenesulfonic Acid Small molecular drug DB08254
2-propionyl-1h-indole-6-carboxamidine Small molecular drug D0Z7YI
4-(3,4-diethoxy-benzylamino)-benzamidine Small molecular drug D0CT8A
4-(4-benzyloxy-3-methoxy-benzylamino)-benzamidine Small molecular drug D02XPB
4-(5-nitro-indol-1-ylmethyl)-benzamidine Small molecular drug D08OCL
4-indol-1-ylmethyl-benzamidine Small molecular drug D0N1PW
4-iodobenzo[B]Thiophene-2-carboxamidine Small molecular drug DB03136
6-styryl-naphthalene-2-carboxamidine Small molecular drug D00POF
8-bromo-6-styryl-naphthalene-2-carboxamidine Small molecular drug D0S4MQ
8-furan-3-yl-6-styryl-naphthalene-2-carboxamidine Small molecular drug D0K0GU
Aminomethylcyclohexane Small molecular drug DB02435
Benzamidine Small molecular drug D07SFI
Camostat Small molecular drug DB13729
Cra_10655 Small molecular drug DB02526
Cra_1144 Small molecular drug DB03643
Cra_8696 Small molecular drug DB03159
Cvs-2139 Small molecular drug D0O0GT
Cvs-2359 Small molecular drug D0C1TS
Diminazene Small molecular drug DB03608
Gabexate Small molecular drug DB12831
Grassystatin A Small molecular drug D0Y5IQ
Hemi-babim Small molecular drug DB01767
L-375378 Small molecular drug D02NHS
Macrocyclic Tripeptide Motif Small molecular drug D0RQ2T
Monoisopropylphosphorylserine Small molecular drug DB01805
Nafamostat Small molecular drug DB12598
Phenethylamine Small molecular drug DB04325
Piperidine-1-carboxamidine Small molecular drug D0M1LO
Pmid3514912c9 Small molecular drug D0F9YV
Rwj-50353 Small molecular drug D09OBJ
Tert-butyloxy Carbonyl-d-phe-pro-arg-h Small molecular drug D03ZUM
Thieno[23-b]Pyridine-2-carboxamidine Small molecular drug DB03876
(1r2s)-2-phenylcyclopropanaminium . DB02665
(2s3r)-2-[[4-(Tert-butylcarbamoyl)Piperazine-1-carbonyl]Amino]-6-(Diaminomethylideneamino)-3-formylhexanoic Acid . DB03417
(S)-n-(4-carbamimidoylbenzyl)-1-(2-(Cyclohexylamino)Ethanoyl)Pyrrolidine-2-carboxamide . DB06850
(S)-n-(4-carbamimidoylbenzyl)-1-(2-(Cyclohexyloxy)Ethanoyl)Pyrrolidine-2-carboxamide . DB07091
(S)-n-(4-carbamimidoylbenzyl)-1-(2-(Cyclopentylamino)Ethanoyl)Pyrrolidine-2-carboxamide . DB06845
(S)-n-(4-carbamimidoylbenzyl)-1-(2-(Cyclopentyloxy)Ethanoyl)Pyrrolidine-2-carboxamide . DB07088
(S)-n-(4-carbamimidoylbenzyl)-1-(3-cyclohexylpropanoyl)Pyrrolidine-2-carboxamide . DB07131
(S)-n-(4-carbamimidoylbenzyl)-1-(3-cyclopentylpropanoyl)Pyrrolidine-2-carboxamide . DB07095
+/-methyl 4-(Aminoiminomethyl)-beta-[3- Inh (Aminoimino)Phenyl]Benzene Pentanoate . DB07985
1-(2-amidinophenyl)-3-(Phenoxyphenyl)Urea . DB03337
1-(4-amidinophenyl)-3-(4-chlorophenyl)Urea . DB04336
1-{[1-(2-amino-3-phenyl-propionyl)-pyrrolidine-2-carbonyl]-amino}-2-(3-cyano-phenyl)-ethaneboronic Acid . DB08420
14:36-dianhydro-2-o-(3-carbamimidoylphenyl)-5-o-(4-carbamimidoylphenyl)-d-glucitol . DB04793
2-(2-hydroxy-5-methoxy-phenyl)-1h-benzoimidazole-5-carboxamidine . DB01905
2-(2-hydroxy-phenyl)-3h-benzoimidazole-5-carboxamidine . DB02287
2-(2-methylphenyl)-1h-indole-5-carboximidamide . DB08184
2-(2-methylphenyl)-1h-indole-6-carboximidamide . DB06918
2-(3-methylphenyl)-1h-indole-5-carboximidamide . DB06923
2-o-(4'-amidinophenyl)-5-o-(3''-amidinophenyl)-14:36-dianhydro-d-sorbitol . DB04791
2-{2-hydroxy-[11'-biphenyl]-3-yl}-1h-13-benzodiazole-5-carboximidamide . DB01725
25-bis-o-{3-[Amino(Imino)Methyl]Phenyl}-14:36-dianhydro-d-glucitol . DB04790
25-oo-bis-{4'4''-amidinophenyl}-14:36-dianhydro-d-sorbitol . DB04792
2h-benzimidazol-2-amine . DB01665
3-phenylpropylamine . DB04410
3-{5-[Amino(Iminio)Methyl]-1h-indol-2-yl}-5-methoxy-11'-biphenyl-2-olate . DB07229
35-diiodotyrosine . DB03374
4-(Methylsulfonyl)Benzenecarboximidamide . DB07368
4-fluorobenzylamine . DB03243
4-phenylbutylamine . DB04311
4-piperidin-4-ylbutanal . DB04654
4-{[1-methyl-5-(2-methyl-benzoimidazol-1-ylmethyl)-1h-benzoimidazol-2-ylmethyl]-amino}-benzamidine . DB02354
5-amidino-benzimidazole . DB01939
5-amino-246-tribromobenzene-13-dicarboxylic Acid . DB07491
6-chloro-2-(2-hydroxy-biphenyl-3-yl)-1h-indole-5-carboxamidine . DB03865
6-fluoro-2-(2-hydroxy-3-isobutoxy-phenyl)-1h-benzoimidazole-5-carboxamidine . DB06855
Aeruginosin 98-b . DB04391
Amylamine . DB02045
Atf-hi-8 . D05ABK
Benzo[B]Thiophene-2-carboxamidine . DB04446
Benzylamine . DB02464
Bis(5-amidino-2-benzimidazolyl)Methane Ketone . DB03213
Bis(5-amidino-2-benzimidazolyl)Methane Ketone Hydrate . DB04301
Bis(5-amidino-2-benzimidazolyl)Methanone . DB01876
Bis(5-amidino-benzimidazolyl)Methane . DB01705
Bis(5-amidino-benzimidazolyl)Methanone Zinc . DB03443
Bis-benzamidine . DB02081
Cra-9334 . DB02288
Cra_10433 . DB03173
Cra_10656 . DB04470
Cra_10762 . DB02366
Cra_10972 . DB02989
Cra_10991 . DB01771
Cra_11092 . DB03555
Cra_16847 . DB02063
Cra_17312 . DB02084
Cra_17693 . DB01741
Cra_1801 . DB03016
Cra_1802 . DB02875
Cra_23653 . DB04246
Cra_9076 . DB04215
Cra_9678 . DB04563
Cra_9785 . DB03595
Cyclotheonamide A . DB04269
Diethyl [(1r)-15-diaminopentyl]Boronate . DB06840
Gr-133686 . D07IBU
Imino[2-(2-oxo-12-dihydro-3-pyridinyl)-1h-benzimidazol-5-yl]Methanaminium . DB04442
Jbp-1 . D0JR9V
N-alpha-(2-naphthylsulfonyl)-n(3-amidino-l-phenylalaninyl)-4-acetyl-piperazine . DB04125
N-alpha-(2-naphthylsulfonyl)-n(3-amidino-l-phenylalaninyl)Isopipecolinic Acid Methyl Ester . DB01745
N-alpha-(2-naphthylsulfonyl)-n-(3-amidino-l-phenylalaninyl)-d-pipecolinic Acid . DB04238
N-cycloheptylglycyl-n-(4-carbamimidoylbenzyl)-l-prolinamide . DB06853
N-cyclooctylglycyl-n-(4-carbamimidoylbenzyl)-l-prolinamide . DB06858
Nalpha-(2-naphthylsulfonylglycyl)-3-amidino-dl-phenylalanine-isopropylester . DB01737
Phosphorylisopropane . DB03976
Pop-1 . D08SMN
Recaat, Ppl Therapeutics/Bayer . D08SKX
Rpr128515 . DB04424
Rpr131247 . DB02744
Rwj-51084 . DB03251
Zinc,[Amino-[2-[[5-[Amino(Azaniumylidene)Methyl]Benzimidazol-1-id-2-yl]Methyl]Benzimidazol-1-id-5-yl]Methylidene]Azanium . DB04008
Zk-805623 . DB04432
Zk-806450 . DB02112
Zk-806711 . DB03373
[(1-{2[(4-carbamimidoyl-phenylamino)-methyl]-1-methyl-1h-benzoimidazol-5-yl}-cyclopropyl)-pyridin-2-yl-methyleneaminooxy]-acetic Acid Ethyl Ester . DB04107
[4-(6-chloro-naphthalene-2-sulfonyl)-piperazin-1-yl]-(3456-tetrahydro-2h-[14']Bipyridinyl-4-yl)-methanone . DB01836
[4-({[5-benzyloxy-1-(3-carbamimidoyl-benzyl)-1h-indole-2-carbonyl]-amino}-methyl)-phenyl]-trimethyl-ammonium . DB02269
[N-(Benzyloxycarbonyl)Amino](4-amidinophenyl)Methane-phosphonate . DB08763
[N-[N-(4-methoxy-236-trimethylphenylsulfonyl)-l-aspartyl]-d-(4-amidino-phenylalanyl)]-piperidine . DB03081
Discontinued
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bmy-44621 Small molecular drug D0GR2H
Dermolastin Small molecular drug D0B9EH
Patamostat Small molecular drug D0CV7T
Rwj-56423 Small molecular drug D05QMJ

References

1 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.