Reaction Details |
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Target | Protein kinase C alpha type |
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Ligand | BDBM50455589 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1754792 (CHEMBL4189552) |
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IC50 | 280±n/a nM |
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Citation | Kwiatkowski, J; Liu, B; Tee, DHY; Chen, G; Ahmad, NHB; Wong, YX; Poh, ZY; Ang, SH; Tan, ESW; Ong, EH; Nurul Dinie, na; Poulsen, A; Pendharkar, V; Sangthongpitag, K; Lee, MA; Sepramaniam, S; Ho, SY; Cherian, J; Hill, J; Keller, TH; Hung, AW Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors. J Med Chem61:4386-4396 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C alpha type |
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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
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BDBM50455589 |
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n/a |
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Name | BDBM50455589 |
Synonyms: | CHEMBL4213984 |
Type | Small organic molecule |
Emp. Form. | C23H19N5O |
Mol. Mass. | 381.4299 |
SMILES | COc1cc2CNCc2cc1-n1cnc2ccc(cc12)-c1ccnc2[nH]ccc12 |
Structure |
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