Target
Protein kinase C iota type
Ligand
BDBM218805
Substrate
n/a
Meas. Tech.
PKC AlphaScreen Assay
pH
7.4±n/a
IC50
4.32e+4± 2e+2 nM
Comments
extracted
Citation
 Arencibia, JMFröhner, WKrupa, MPastor-Flores, DMerker, POellerich, TNeimanis, SSchmithals, CKöberle, VSüß, EZeuzem, SStark, HPiiper, AOdadzic, DSchulze, JOBiondi, RM An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms. ACS Chem Biol 12:564-573 (2017) [PubMed]  Article 
Target
Name:
Protein kinase C iota type
Synonyms:
Atypical protein kinase C-lambda/iota | DXS1179E | KPCI_HUMAN | PRKC-lambda/iota | PRKCI | Protein kinase C (PKC) | Protein kinase C iota | Protein kinase C iota (PKCι) | Protein kinase C iota type | Protein kinase C iota type/zeta type | aPKC-lambda/iota | nPKC-iota
Type:
Enzyme
Mol. Mass.:
68251.56
Organism:
Homo sapiens (Human)
Description:
P41743
Residue:
596
Sequence:
MPTQRDSSTMSHTVAGGGSGDHSHQVRVKAYYRGDIMITHFEPSISFEGLCNEVRDMCSFDNEQLFTMKWIDEEGDPCTVSSQLELEEAFRLYELNKDSELLIHVFPCVPERPGMPCPGEDKSIYRRGARRWRKLYCANGHTFQAKRFNRRAHCAICTDRIWGLGRQGYKCINCKLLVHKKCHKLVTIECGRHSLPQEPVMPMDQSSMHSDHAQTVIPYNPSSHESLDQVGEEKEAMNTRESGKASSSLGLQDFDLLRVIGRGSYAKVLLVRLKKTDRIYAMKVVKKELVNDDEDIDWVQTEKHVFEQASNHPFLVGLHSCFQTESRLFFVIEYVNGGDLMFHMQRQRKLPEEHARFYSAEISLALNYLHERGIIYRDLKLDNVLLDSEGHIKLTDYGMCKEGLRPGDTTSTFCGTPNYIAPEILRGEDYGFSVDWWALGVLMFEMMAGRSPFDIVGSSDNPDQNTEDYLFQVILEKQIRIPRSLSVKAASVLKSFLNKDPKERLGCHPQTGFADIQGHPFFRNVDWDMMEQKQVVPPFKPNISGEFGLDNFDSQFTNEPVQLTPDDDDIVRKIDQSEFEGFEYINPLLMSAEECV
  
Inhibitor
Name:
BDBM218805
Synonyms:
PS212
Type:
Small organic molecule
Emp. Form.:
C20H15Cl2N3O4
Mol. Mass.:
432.257
SMILES:
CCOC(=O)C1=C(O)C(=O)N(C1c1ccc(Cl)cc1)c1nc2ccc(Cl)cc2[nH]1 |c:5|
Structure:
Search PDB for entries with ligand similarity: