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Target
Kallikrein-5
Ligand
BDBM50459539
Substrate
n/a
Meas. Tech.
ChEMBL_1766595 (CHEMBL4201842)
IC50
130±n/a nM
Citation
 De Vita, E; Schüler, P; Lovell, S; Lohbeck, J; Kullmann, S; Rabinovich, E; Sananes, A; Heßling, B; Hamon, V; Papo, N; Hess, J; Tate, EW; Gunkel, N; Miller, AK Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. J Med Chem 61:8859-8874 (2018) [PubMed]  Article
Target
Name:
Kallikrein-5
Synonyms:
KLK5 | KLK5_HUMAN | Kallikrein 5 | SCTE | kallikrein-related peptidase 5 preproprotein
Type:
PROTEIN
Mol. Mass.:
32031.72
Organism:
Homo sapiens (Human)
Description:
EBI_12584
Residue:
293
Sequence:
MATARPPWMWVLCALITALLLGVTEHVLANNDVSCDHPSNTVPSGSNQDLGAGAGEDARSDDSSSRIINGSDCDMHTQPWQAALLLRPNQLYCGAVLVHPQWLLTAAHCRKKVFRVRLGHYSLSPVYESGQQMFQGVKSIPHPGYSHPGHSNDLMLIKLNRRIRPTKDVRPINVSSHCPSAGTKCLVSGWGTTKSPQVHFPKVLQCLNISVLSQKRCEDAYPRQIDDTMFCAGDKAGRDSCQGDSGGPVVCNGSLQGLVSWGDYPCARPNRPGVYTNLCKFTKWIQETIQANS
  
Inhibitor
Name:
BDBM50459539
Synonyms:
CHEMBL4206734
Type:
Small organic molecule
Emp. Form.:
C25H26N6O3
Mol. Mass.:
458.5123
SMILES:
Cc1nn(c(C)c1NC(=O)COC(=O)Cc1c(C)[nH]c2cc(ccc12)C(N)=N)-c1ccccc1
Structure:
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