General Information of the Protein
Protein ID
PT01697
Protein Name
Calpain-1 catalytic subunit
Secondarily
Protein Name
Calcium-activated neutral proteinase 1
Calpain mu-type
Calpain-1 large subunit
Cell proliferation-inducing gene 30 protein
Micromolar-calpain
Gene Name
CAPN1
Secondarily
Gene Name
CANPL1
PIG30
Sequence
MSEEIITPVYCTGVSAQVQKQRARELGLGRHENAIKYLGQDYEQLRVRCLQSGTLFRDEAFPPVPQSLGYKDLGPNSSKTYGIKWKRPTELLSNPQFIVDGATRTDICQGALGDCWLLAAIASLTLNDTLLHRVVPHGQSFQNGYAGIFHFQLWQFGEWVDVVVDDLLPIKDGKLVFVHSAEGNEFWSALLEKAYAKVNGSYEALSGGSTSEGFEDFTGGVTEWYELRKAPSDLYQIILKALERGSLLGCSIDISSVLDMEAITFKKLVKGHAYSVTGAKQVNYRGQVVSLIRMRNPWGEVEWTGAWSDSSSEWNNVDPYERDQLRVKMEDGEFWMSFRDFMREFTRLEICNLTPDALKSRTIRKWNTTLYEGTWRRGSTAGGCRNYPATFWVNPQFKIRLDETDDPDDYGDRESGCSFVLALMQKHRRRERRFGRDMETIGFAVYEVPPELVGQPAVHLKRDFFLANASRARSEQFINLREVSTRFRLPPGEYVVVPSTFEPNKEGDFVLRFFSEKSAGTVELDDQIQANLPDEQVLSEEEIDENFKALFRQLAGEDMEISVKELRTILNRIISKHKDLRTKGFSLESCRSMVNLMDRDGNGKLGLVEFNILWNRIRNYLSIFRKFDLDKSGSMSAYEMRMAIESAGFKLNKKLYELIITRYSEPDLAVDFDNFVCCLVRLETMFRFFKTLDTDLDGVVTFDLFKWLQLTMFA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Cysteine protease
>
Cysteine protease CA clan
>
Cysteine protease C2 family
Function
Calcium-regulated non-lysosomal thiol-protease which catalyzes limited proteolysis of substrates involved in cytoskeletal remodeling and signal transduction (PubMed:19617626, PubMed:21531719, PubMed:2400579). Proteolytically cleaves CTBP1 at 'Asn-375', 'Gly-387' and 'His-409' (PubMed:23707407). Cleaves and activates caspase-7 (CASP7) (PubMed:19617626).
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Uniprot ID
Primary ID:
P07384

Secondarily ID:
Q2TTR0
Q6DHV4
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Ensembl ID
ENSG00000014216
HGNC ID
HGNC:1476
Subcellular Location
Cytoplasm
Cell membrane
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: CL000116 , MOLT-4
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0192820
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid ((S)-1-benzyl-2-butylcarbamoyl-2-oxo-ethyl)-amide
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C27H33N3O7S
  1
1
IC50 = 2.1 nM
 Bioactivity Info 
   TI
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CP0048127
 Compound Info 
(3S) 2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C22H24N2O6S
  1
1
IC50 = 500 nM
 Bioactivity Info 
   TI
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CP0342893
 Compound Info 
2-Methyl-1,1-dioxo-1,2,6,7-tetrahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C21H20N2O6S
  1
1
IC50 = 900 nM
 Bioactivity Info 
   TI
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CP0148043
 Compound Info 
6,7-Dichloro-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C19H18Cl2N2O4S
  1
1
IC50 = 1300 nM
 Bioactivity Info 
   TI
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CP0172119
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-oxo-2-[2-(5-pyridin-2-yl-thiophene-2-sulfonylamino)-ethylcarbamoyl]-ethyl}-amide
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C34H35N5O9S3
  1
1
IC50 = 1300 nM
 Bioactivity Info 
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CP0177716
 Compound Info 
2-Methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C19H20N2O4S
  1
1
IC50 = 1700 nM
 Bioactivity Info 
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CP0168893
 Compound Info 
2-Methyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (5-benzenesulfonylamino-1-formyl-pentyl)-amide
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C24H29N3O8S2
  1
1
IC50 = 1800 nM
 Bioactivity Info 
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CP0185518
 Compound Info 
6,7-Dimethoxy-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C21H24N2O6S
  1
1
IC50 = 1900 nM
 Bioactivity Info 
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CP0362027
 Compound Info 
2-Methyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C21H22N2O6S
  1
1
IC50 = 2000 nM
 Bioactivity Info 
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CP0290024
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[2-(4-fluoro-benzenesulfonylamino)-ethylcarbamoyl]-2-oxo-ethyl}-amide
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C31H33FN4O9S2
  1
1
IC50 = 2000 nM
 Bioactivity Info 
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CP0207897
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,6,7-tetrahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid ((S)-1-benzyl-2-oxo-ethyl)-amide
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C22H22N2O6S
  1
1
IC50 = 2100 nM
 Bioactivity Info 
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CP0063942
 Compound Info 
6-Chloro-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C19H19ClN2O4S
  1
1
IC50 = 2200 nM
 Bioactivity Info 
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CP0133619
 Compound Info 
6,7-Dimethoxy-1,1-dioxo-3,4-dihydro-1H-1lambda*6*-benzo[c][1,2]oxathiine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C20H21NO7S
  1
1
IC50 = 2200 nM
 Bioactivity Info 
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CP0370357
 Compound Info 
6-Fluoro-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C19H19FN2O4S
  1
1
IC50 = 2400 nM
 Bioactivity Info 
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CP0288520
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[3-(4-fluoro-benzenesulfonylamino)-propylcarbamoyl]-2-oxo-ethyl}-amide
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C32H35FN4O9S2
  1
1
IC50 = 2400 nM
 Bioactivity Info 
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CP0184142
 Compound Info 
2-Isopropyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C23H26N2O6S
  1
1
IC50 = 2600 nM
 Bioactivity Info 
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CP0193881
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid [(S)-2-(3-benzenesulfonylamino-propylcarbamoyl)-1-benzyl-2-oxo-ethyl]-amide
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C32H36N4O9S2
  1
1
IC50 = 2700 nM
 Bioactivity Info 
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CP0084259
 Compound Info 
6,7-Dichloro-2-methyl-1,1-dioxo-1,2-dihydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C19H16Cl2N2O4S
  1
1
IC50 = 2900 nM
 Bioactivity Info 
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CP0048650
 Compound Info 
4-Methoxy-2-methyl-1,1-dioxo-1,2-dihydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C20H20N2O5S
  1
1
IC50 = 3200 nM
 Bioactivity Info 
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CP0272619
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[3-(4-nitro-benzenesulfonylamino)-propylcarbamoyl]-2-oxo-ethyl}-amide
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C32H35N5O11S2
  1
1
IC50 = 3600 nM
 Bioactivity Info 
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CP0147827
 Compound Info 
2-Methyl-6-morpholin-4-yl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C23H27N3O5S
  1
1
IC50 = 4100 nM
 Bioactivity Info 
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CP0208488
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[2-(4-nitro-benzenesulfonylamino)-ethylcarbamoyl]-2-oxo-ethyl}-amide
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C31H33N5O11S2
  1
1
IC50 = 4200 nM
 Bioactivity Info 
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CP0272483
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid [(S)-2-(2-benzenesulfonylamino-ethylcarbamoyl)-1-benzyl-2-oxo-ethyl]-amide
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C31H34N4O9S2
  1
1
IC50 = 5000 nM
 Bioactivity Info 
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CP0113102
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-formyl-3-methyl-butyl)-amide
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C19H26N2O6S
  1
1
IC50 > 3000 nM
 Bioactivity Info 
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0342893
 Compound Info 
2-Methyl-1,1-dioxo-1,2,6,7-tetrahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C21H20N2O6S
  1
1 IC50 = 6 nM
CP0048127
 Compound Info 
(3S) 2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C22H24N2O6S
  1
1 IC50 = 7 nM
CP0207897
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,6,7-tetrahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid ((S)-1-benzyl-2-oxo-ethyl)-amide
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C22H22N2O6S
  1
1 IC50 = 8 nM
CP0084259
 Compound Info 
6,7-Dichloro-2-methyl-1,1-dioxo-1,2-dihydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C19H16Cl2N2O4S
  1
1 IC50 = 15 nM
CP0172119
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-oxo-2-[2-(5-pyridin-2-yl-thiophene-2-sulfonylamino)-ethylcarbamoyl]-ethyl}-amide
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C34H35N5O9S3
  1
1 IC50 = 20 nM
CP0040174
 Compound Info 
1-Benzyl-2,3-dihydro-1H-indole-5-carboxylic acid [(S)-1-((S)-2-hydroxy-tetrahydro-furan-3-ylcarbamoyl)-3-methyl-butyl]-amide
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C26H33N3O4
  1
1 IC50 = 20 nM
CP0146592
 Compound Info 
N-[(2S)-1-[[(3S)-2-hydroxyoxolan-3-yl]amino]-4-methyl-1-oxopentan-2-yl]-10H-phenothiazine-2-carboxamide
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C23H27N3O4S
  1
1 IC50 = 22.5 nM
CP0362027
 Compound Info 
2-Methyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C21H22N2O6S
  1
1 IC50 = 24 nM
CP0370357
 Compound Info 
6-Fluoro-2-methyl-1,1-dioxo-1,2,3,4-tetrahydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C19H19FN2O4S
  1
1 IC50 = 28 nM
CP0290024
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[2-(4-fluoro-benzenesulfonylamino)-ethylcarbamoyl]-2-oxo-ethyl}-amide
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C31H33FN4O9S2
  1
1 IC50 = 29 nM
CP0184142
 Compound Info 
2-Isopropyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C23H26N2O6S
  1
1 IC50 = 30 nM
CP0193881
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid [(S)-2-(3-benzenesulfonylamino-propylcarbamoyl)-1-benzyl-2-oxo-ethyl]-amide
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C32H36N4O9S2
  1
1 IC50 = 35 nM
CP0048650
 Compound Info 
4-Methoxy-2-methyl-1,1-dioxo-1,2-dihydro-1lambda*6*-benzo[e][1,2]thiazine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide
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C20H20N2O5S
  1
1 IC50 = 37 nM
CP0272483
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid [(S)-2-(2-benzenesulfonylamino-ethylcarbamoyl)-1-benzyl-2-oxo-ethyl]-amide
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C31H34N4O9S2
  1
1 IC50 = 40 nM
CP0208488
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[2-(4-nitro-benzenesulfonylamino)-ethylcarbamoyl]-2-oxo-ethyl}-amide
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C31H33N5O11S2
  1
1 IC50 = 47 nM
CP0272619
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[3-(4-nitro-benzenesulfonylamino)-propylcarbamoyl]-2-oxo-ethyl}-amide
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C32H35N5O11S2
  1
1 IC50 = 50 nM
CP0288520
 Compound Info 
2-Ethyl-1,1-dioxo-1,2,3,4,6,7-hexahydro-5,8-dioxa-1lambda*6*-thia-2-aza-anthracene-3-carboxylic acid {(S)-1-benzyl-2-[3-(4-fluoro-benzenesulfonylamino)-propylcarbamoyl]-2-oxo-ethyl}-amide
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C32H35FN4O9S2
  1
1 IC50 = 50 nM
CP0133619
 Compound Info 
6,7-Dimethoxy-1,1-dioxo-3,4-dihydro-1H-1lambda*6*-benzo[c][1,2]oxathiine-3-carboxylic acid (1-benzyl-2-oxo-ethyl)-amide(3R,3S diastereomeric mixture)
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C20H21NO7S
  1
1 IC50 = 51 nM
Clinical Information about the Protein
Target 1 ( Calpain-1 (CAPN1) )
Target Type Patented-recorded Target