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Target
Caspase-8
Ligand
BDBM50160973
Substrate
n/a
Meas. Tech.
ChEMBL_305653 (CHEMBL829511)
IC50
6.6±n/a nM
Citation
 Han, Y; Giroux, A; Colucci, J; Bayly, CI; Mckay, DJ; Roy, S; Xanthoudakis, S; Vaillancourt, J; Rasper, DM; Tam, J; Tawa, P; Nicholson, DW; Zamboni, RJ Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors. Bioorg Med Chem Lett 15:1173-80 (2005) [PubMed]  Article 
Target
Name:
Caspase-8
Synonyms:
Apoptotic cysteine protease | Apoptotic protease Mch-5 | CAP4 | CASP-8 | CASP8 | CASP8_HUMAN | Caspase | Caspase-8 subunit p10 | Caspase-8 subunit p18 | FADD-homologous ICE/CED-3-like protease | FADD-like ICE | FLICE | ICE-like apoptotic protease 5 | MACH | MCH5 | MORT1-associated CED-3 homolog
Type:
Enzyme
Mol. Mass.:
55373.89
Organism:
Homo sapiens (Human)
Description:
Q14790
Residue:
479
Sequence:
MDFSRNLYDIGEQLDSEDLASLKFLSLDYIPQRKQEPIKDALMLFQRLQEKRMLEESNLSFLKELLFRINRLDLLITYLNTRKEEMERELQTPGRAQISAYRVMLYQISEEVSRSELRSFKFLLQEEISKCKLDDDMNLLDIFIEMEKRVILGEGKLDILKRVCAQINKSLLKIINDYEEFSKERSSSLEGSPDEFSNGEELCGVMTISDSPREQDSESQTLDKVYQMKSKPRGYCLIINNHNFAKAREKVPKLHSIRDRNGTHLDAGALTTTFEELHFEIKPHDDCTVEQIYEILKIYQLMDHSNMDCFICCILSHGDKGIIYGTDGQEAPIYELTSQFTGLKCPSLAGKPKVFFIQACQGDNYQKGIPVETDSEEQPYLEMDLSSPQTRYIPDEADFLLGMATVNNCVSYRNPAEGTWYIQSLCQSLRERCPRGDDILTILTEVNYEVSNKDDKKNMGKQMPQPTFTLRKKLVFPSD
  
Inhibitor
Name:
BDBM50160973
Synonyms:
(S)-5-Benzylsulfanyl-4-oxo-3-(2-{2-oxo-3-[(thiazol-5-ylmethyl)-amino]-2H-pyrazin-1-yl}-butyrylamino)-pentanoic acid | CHEMBL180273
Type:
Small organic molecule
Emp. Form.:
C24H27N5O5S2
Mol. Mass.:
529.632
SMILES:
CCC(C(=O)N[C@@H](CC(O)=O)C(=O)CSCc1ccccc1)n1ccnc(NCc2cncs2)c1=O
Structure:
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