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Target
Protein kinase C alpha type
Ligand
BDBM3033
Substrate
n/a
Meas. Tech.
ChEMBL_650126 (CHEMBL1219824)
IC50
3.7±n/a nM
Citation
 Meredith, EL; Ardayfio, O; Beattie, K; Dobler, MR; Enyedy, I; Gaul, C; Hosagrahara, V; Jewell, C; Koch, K; Lee, W; Lehmann, H; McKinsey, TA; Miranda, K; Pagratis, N; Pancost, M; Patnaik, A; Phan, D; Plato, C; Qian, M; Rajaraman, V; Rao, C; Rozhitskaya, O; Ruppen, T; Shi, J; Siska, SJ; Springer, C; van Eis, M; Vega, RB; von Matt, A; Yang, L; Yoon, T; Zhang, JH; Zhu, N; Monovich, LG Identification of orally available naphthyridine protein kinase D inhibitors. J Med Chem 53:5400-21 (2010) [PubMed]  Article 
Target
Name:
Protein kinase C alpha type
Synonyms:
KPCA_HUMAN | PKC alpha | PKC alpha and beta-2 | PKC-A | PKC-alpha | PKCA | PRKACA | PRKCA | Protein Kinase C- alpha | Protein kinase C alpha | Protein kinase C alpha (PKCa) | Protein kinase C alpha type (PKC-A) | Protein kinase C alpha type (PRKCA) | Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase
Type:
Enzyme
Mol. Mass.:
76755.65
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
672
Sequence:
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGSLLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDAKNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRLSVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNMELRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKGTEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYVNGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIADFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDGEDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRIDWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVNPQFVHPILQSAV
  
Inhibitor
Name:
BDBM3033
Synonyms:
3-{23-methyl-14-oxo-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17,19,21-nonaen-3-yl}propanenitrile | CHEMBL302449 | Go 6976 | Indolocarbazole deriv.
Type:
Small organic molecule
Emp. Form.:
C24H18N4O
Mol. Mass.:
378.4259
SMILES:
Cn1c2ccccc2c2c3C(=O)NCc3c3c4ccccc4n(CCC#N)c3c12
Structure:
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