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Target
Protein kinase C alpha type
Ligand
BDBM25018
Substrate
n/a
Meas. Tech.
ChEMBL_438493 (CHEMBL887593)
IC50
466000±n/a nM
Citation
Hayakawa, M; Kaizawa, H; Moritomo, H; Koizumi, T; Ohishi, T; Yamano, M; Okada, M; Ohta, M; Tsukamoto, S; Raynaud, FI; Workman, P; Waterfield, MD; Parker, P Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem Lett 17:2438-42 (2007) [PubMed] Article
More Info.:
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:
BDBM25018
Synonyms:
3-(4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)phenol | 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol | CHEMBL541643 | thieno[3,2-d]pyrimidine derivative, 1 | thienopyrimidine derivative, 1
Type:
Small organic molecule
Emp. Form.:
C16H15N3O2S
Mol. Mass.:
313.374
SMILES:
Oc1cccc(c1)-c1nc(N2CCOCC2)c2sccc2n1