Reaction Details |
| Report a problem with these data |
Target | Protein kinase C alpha type |
---|
Ligand | BDBM50387353 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_828100 (CHEMBL2049839) |
---|
Ki | >1250±n/a nM |
---|
Citation | Jimenez, JM; Davis, C; Boyall, D; Fraysse, D; Knegtel, R; Settimo, L; Young, S; Bolton, C; Chiu, P; Curnock, A; Rasmussen, R; Tanner, A; Ager, I Structure-based optimization of aminopyridines as PKC¿ inhibitors. Bioorg Med Chem Lett22:4645-9 (2012) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Protein kinase C alpha type |
---|
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: | MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
|
|
|
BDBM50387353 |
---|
n/a |
---|
Name | BDBM50387353 |
Synonyms: | CHEMBL2046650 |
Type | Small organic molecule |
Emp. Form. | C26H31N5O |
Mol. Mass. | 429.5572 |
SMILES | CC(C)C[C@H]1CN(CCN1)c1ccc(Cc2ccccc2)c(n1)C(=O)c1cccnc1N |r| |
Structure |
|