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Literature summary for 3.4.22.15 extracted from

  • Parker, E.N.; Song, J.; Kishore Kumar, G.D.; Odutola, S.O.; Chavarria, G.E.; Charlton-Sevcik, A.K.; Strecker, T.E.; Barnes, A.L.; Sudhan, D.R.; Wittenborn, T.R.; Siemann, D.W.; Horsman, M.R.; Chaplin, D.J.; Trawick, M.L.; Pinney, K.G.
    Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L (2015), Bioorg. Med. Chem., 23, 6974-6992 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.15

Inhibitors

Inhibitors Comment Organism Structure
(2-fluorobenzophenone) thiosemicarbazone
-
 Homo sapiens
(2E)-2-(6-bromo-1,1-dioxido-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
 Homo sapiens
(2E)-2-(6-bromo-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
 Homo sapiens
(2E)-2-(6-bromo-2,3-dihydroquinolin-4(1H)-ylidene)hydrazinecarbothioamide
-
 Homo sapiens
(2E)-2-(6-nitro-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
 Homo sapiens
(2E)-2-[6-(propan-2-yloxy)-2,3-dihydro-4H-thiochromen-4-ylidene]hydrazinecarbothioamide
-
 Homo sapiens
(3-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
-
 Homo sapiens
(3-bromo-3'-hydroxybenzophenone) thiosemicarbazone a slowly reversible inhibitor of cathepsin L Homo sapiens
(3-hydroxybenzophenone) thiosemicarbazone
-
 Homo sapiens
(4-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
-
 Homo sapiens
1,3,5-trisbenzoylbenzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(2-fluorobenzoyl)-5-bromobenzene thiosemicarbazone molecular docking in the active site Homo sapiens
1,3-bis(3-bromobenzoyl)-5-bromobenzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(3-bromobenzoyl)-5-hydroxybenzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(3-hydroxybenzoyl)-5-bromobenzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(3-methylbenzoyl)benzene thisosemicarbazone
-
 Homo sapiens
1,3-bis(4-bromobenzoyl)benzene bis-thiosemicarbazone
-
 Homo sapiens
1,3-bis(4-bromobenzoyl)benzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(4-fluorobenzoyl)benzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(4-hydroxybenzoyl)benzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(4-isopropoxybenzoyl)benzene thiosemicarbazone
-
 Homo sapiens
1,3-bis(4-methoxybenzoyl)benzene thiosemicarbazone
-
 Homo sapiens
3-benzoylbenzhydrol thiosemicarbazone
-
 Homo sapiens
benzophenone thiosemicarbazone
-
 Homo sapiens
benzoylbenzophenone thiosemicarbazone molecular docking in the active site Homo sapiens
additional information synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L, molecular modeling, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P07711
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MDA-MB-231 cell
-
 Homo sapiens
-
PC-3ML cell
-
 Homo sapiens
-
prostate gland cancer cell
-
 Homo sapiens
-
umbilical vein endothelial cell HUVEC Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-L-Arg-L-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-L-Arg-L-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
cathepsin L1
-
 Homo sapiens
CatL
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000081
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(2-fluorobenzoyl)-5-bromobenzene thiosemicarbazone
0.0000099
-
 pH 6.0, 37°C Homo sapiens benzoylbenzophenone thiosemicarbazone
0.0000144
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(4-fluorobenzoyl)benzene thiosemicarbazone
0.0000238
-
 pH 6.0, 37°C Homo sapiens 3-benzoylbenzhydrol thiosemicarbazone
0.0000305
-
 pH 6.0, 37°C Homo sapiens (3-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
0.000056
-
 pH 6.0, 37°C Homo sapiens 1,3,5-trisbenzoylbenzene thiosemicarbazone
0.000068
-
 pH 6.0, 37°C Homo sapiens (2E)-2-(6-nitro-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
0.0000716
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(3-hydroxybenzoyl)-5-bromobenzene thiosemicarbazone
0.0001314
-
 pH 6.0, 37°C Homo sapiens (3-bromo-3'-hydroxybenzophenone) thiosemicarbazone
0.000152
-
 pH 6.0, 37°C Homo sapiens (2E)-2-(6-bromo-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
0.000164
-
 pH 6.0, 37°C Homo sapiens (2E)-2-(6-bromo-2,3-dihydroquinolin-4(1H)-ylidene)hydrazinecarbothioamide
0.00034
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(4-hydroxybenzoyl)benzene thiosemicarbazone
0.000574
-
 pH 6.0, 37°C Homo sapiens (2E)-2-(6-bromo-1,1-dioxido-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
0.000654
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(3-methylbenzoyl)benzene thisosemicarbazone
0.001522
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(4-bromobenzoyl)benzene thiosemicarbazone
0.00222
-
 pH 6.0, 37°C Homo sapiens (4-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
0.005117
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(4-methoxybenzoyl)benzene thiosemicarbazone
0.01
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(3-bromobenzoyl)-5-hydroxybenzene thiosemicarbazone
0.01
-
 above, pH 6.0, 37°C Homo sapiens (2-fluorobenzophenone) thiosemicarbazone
0.01
-
 above, pH 6.0, 37°C Homo sapiens (2E)-2-[6-(propan-2-yloxy)-2,3-dihydro-4H-thiochromen-4-ylidene]hydrazinecarbothioamide
0.01
-
 above, pH 6.0, 37°C Homo sapiens (3-hydroxybenzophenone) thiosemicarbazone
0.01
-
 above, pH 6.0, 37°C Homo sapiens 1,3-bis(4-bromobenzoyl)benzene bis-thiosemicarbazone
0.01
-
 above, pH 6.0, 37°C Homo sapiens 1,3-bis(4-isopropoxybenzoyl)benzene thiosemicarbazone
0.01
-
 above, pH 6.0, 37°C Homo sapiens benzophenone thiosemicarbazone
0.01035
-
 pH 6.0, 37°C Homo sapiens 1,3-bis(3-bromobenzoyl)-5-bromobenzene thiosemicarbazone