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Target
Protein kinase C alpha type
Ligand
BDBM50057511
Substrate
n/a
Meas. Tech.
ChEMBL_160289 (CHEMBL769617)
Ki
11±n/a nM
Citation
 Kozikowski, AP; Wang, S; Ma, D; Yao, J; Ahmad, S; Glazer, RI; Bogi, K; Acs, P; Modarres, S; Lewin, NE; Blumberg, PM Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme selectivity. J Med Chem 40:1316-26 (1997) [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:
BDBM50057511
Synonyms:
(+/-)-indolactum-V 13-Hydroxymethyl-10-isopropyl-9-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4,6,8(15)-tetraen-11-one | (-)-indolactam V | (10S,13S)-13-Hydroxymethyl-10-isopropyl-9-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4(15),5,7-tetraen-11-one | (10S,13S)-13-Hydroxymethyl-10-isopropyl-9-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4,6,8(15)-tetraen-11-one | (2S,5S)-5-(hydroxymethyl)-2-isopropyl-1-methyl-1,2,5,6-tetrahydro-4H-[1,4]diazonino[7,6,5-cd]indol-3(8H)-one | (S)-13-Hydroxymethyl-10-isopropyl-9-(S)-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4,6,8(15)-tetraen-11-one | 13-Hydroxymethyl-10-isopropyl-9-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4(15),5,7-tetraen-11-one | 13-Hydroxymethyl-10-isopropyl-9-methyl-3,9,12-triaza-tricyclo[6.6.1.0*4,15*]pentadeca-1,4,6,8(15)-tetraen-11-one(ILV) | CHEMBL27266 | INDOLACTUM | indolactam-V
Type:
Small organic molecule
Emp. Form.:
C17H23N3O2
Mol. Mass.:
301.3834
SMILES:
CC(C)[C@@H]1N(C)c2cccc3[nH]cc(C[C@@H](CO)NC1=O)c23
Structure:
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