serine protease 1 | S1: Chymotrypsin | IUPHAR/BPS Guide to PHARMACOLOGY

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serine protease 1

target has curated data in GtoImmuPdb

Target id: 2397

Nomenclature: serine protease 1

Family: S1: Chymotrypsin

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 247 7q34 PRSS1 serine protease 1
Mouse - 264 6 B1 Prss1 protease, serine 1 (trypsin 1)
Rat - 247 4q22 Prss3b protease, serine, 3B
Previous and Unofficial Names
cationic trypsin-3 | cationic trypsin III | cationic trypsinogen | protease | protease, serine 1 | protease, serine, 1 (trypsin 1) | protease, serine 1 (trypsin 1) | protease, serine, 3 | protease, serine, 3B | Prss3 | Try1 | Try3 | Trygn16 | trypsinogen 16
Database Links
Specialist databases
MEROPS S01.127 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
RWJ-56423 Bt Inhibition 8.1 pKi 1
pKi 8.1 (Ki 8.09x10-9 M) [1]
nafamostat Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.7x10-8 M) [3]
compound 9 [PMID: 3514912] Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 1.95x10-8 M) [4]
camostat Hs Inhibition 7.3 pIC50 5
pIC50 7.3 (IC50 5.06x10-8 M) [5]
View species-specific inhibitor tables
Immunopharmacology Comments
Inhibition of PRSS1 (and TPSAB1), released from mast cells in response to allergen exposure, abrogates the subsequent allergic airway response in vivo [1-2]: e.g. see dual TPSAB1/PRSS1 inhibitor RWJ-58643.
Clinically-Relevant Mutations and Pathophysiology
Disease:  Hereditary pancreatitis
Synonyms: Hereditary chronic pancreatitis [Orphanet: ORPHA676]
OMIM: 167800
Orphanet: ORPHA676
Disease:  Trypsinogen deficiency
OMIM: 614044


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1. Costanzo MJ, Yabut SC, Almond Jr HR, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D et al.. (2003) Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. J. Med. Chem., 46 (18): 3865-76. [PMID:12930148]

2. Erin EM, Leaker BR, Zacharasiewicz A, Higgins LA, Nicholson GC, Boyce MJ, de Boer P, Jones RC, Durham SR, Barnes PJ et al.. (2006) Effects of a reversible beta-tryptase and trypsin inhibitor (RWJ-58643) on nasal allergic responses. Clin. Exp. Allergy, 36 (4): 458-64. [PMID:16630150]

3. Hays SJ, Caprathe BW, Gilmore JL, Amin N, Emmerling MR, Michael W, Nadimpalli R, Nath R, Raser KJ, Stafford D et al.. (1998) 2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. J. Med. Chem., 41 (7): 1060-7. [PMID:9544206]

4. Kaminski JM, Bauer L, Mack SR, Anderson Jr RA, Waller DP, Zaneveld LJ. (1986) Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates. J. Med. Chem., 29 (4): 514-9. [PMID:3514912]

5. Senokuchi K, Nakai H, Nakayama Y, Odagaki Y, Sakaki K, Kato M, Maruyama T, Miyazaki T, Ito H, Kamiyasu K et al.. (1995) New orally active serine protease inhibitors. J. Med. Chem., 38 (14): 2521-3. [PMID:7629790]

How to cite this page

S1: Chymotrypsin: serine protease 1. Last modified on 27/02/2018. Accessed on 12/07/2020. IUPHAR/BPS Guide to PHARMACOLOGY,