Reaction Details |
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Target | Protein kinase C alpha/beta/gamma type |
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Ligand | BDBM50136008 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_162381 (CHEMBL767469) |
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IC50 | >10000±n/a nM |
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Citation | Gingrich, DE; Reddy, DR; Iqbal, MA; Singh, J; Aimone, LD; Angeles, TS; Albom, M; Yang, S; Ator, MA; Meyer, SL; Robinson, C; Ruggeri, BA; Dionne, CA; Vaught, JL; Mallamo, JP; Hudkins, RL A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clin J Med Chem46:5375-88 (2003) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C alpha/beta/gamma type |
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Name: | Protein kinase C alpha/beta/gamma type |
Synonyms: | Protein kinase C, PKC; classical |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 162381 |
Components: | This complex has 3 components. |
Component 1 |
Name: | Protein kinase C alpha type |
Synonyms: | KPCA_RAT | Pkca | Prkca | Protein kinase C (PKC) | Protein kinase C alpha | Protein kinase C alpha type |
Type: | Protein |
Mol. Mass.: | 76797.67 |
Organism: | Rattus norvegicus (Rat) |
Description: | P05696 |
Residue: | 672 |
Sequence: | MADVYPANDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVTDEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNVE
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSICKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
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Component 2 |
Name: | Protein kinase C beta type |
Synonyms: | KPCB_RAT | PKC, rat brain | Pkcb | Prkcb | Prkcb1 | Protein Kinase C | Protein kinase C (PKC) | Protein kinase C beta |
Type: | Enzyme Mixture |
Mol. Mass.: | 76755.54 |
Organism: | Rattus norvegicus (rat) |
Description: | PKC from rat brain is known to contain predominately the conventional PKC isoforms, alpha, beta I, beta II, gamma. |
Residue: | 671 |
Sequence: | MADPAAGPPPSEGEESTVRFARKGALRQKNVHEVKNHKFTARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPASDDPRSKHKFKIHTYSSPTFCDHCGS
LLYGLIHQGMKCDTCMMNVHKRCVMNVPSLCGTDHTERRGRIYIQAHIDREVLIVVVRDA
KNLVPMDPNGLSDPYVKLKLIPDPKSESKQKTKTIKCSLNPEWNETFRFQLKESDKDRRL
SVEIWDWDLTSRNDFMGSLSFGISELQKAGVDGWFKLLSQEEGEYFNVPVPPEGSEGNEE
LRQKFERAKIGQGTKAPEEKTANTISKFDNNGNRDRMKLTDFNFLMVLGKGSFGKVMLSE
RKGTDELYAVKILKKDVVIQDDDVECTMVEKRVLALPGKPPFLTQLHSCFQTMDRLYFVM
EYVNGGDLMYHIQQVGRFKEPHAVFYAAEIAIGLFFLQSKGIIYRDLKLDNVMLDSEGHI
KIADFGMCKENIWDGVTTKTFCGTPDYIAPEIIAYQPYGKSVDWWAFGVLLYEMLAGQAP
FEGEDEDELFQSIMEHNVAYPKSMSKEAVAICKGLMTKHPGKRLGCGPEGERDIKEHAFF
RYIDWEKLERKEIQPPYKPKARDKRDTSNFDKEFTRQPVELTPTDKLFIMNLDQNEFAGF
SYTNPEFVINV
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Component 3 |
Name: | Protein kinase C gamma type |
Synonyms: | KPCG_RAT | Pkcc | Pkcg | Prkcc | Prkcg | Protein kinase C (PKC) | Protein kinase C gamma |
Type: | PROTEIN |
Mol. Mass.: | 78367.88 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_152979 |
Residue: | 697 |
Sequence: | MAGLGPGGGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIG
KQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSL
LYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTSDEIHITVGEA
RNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTKTVKATLNPVWNETFVFNLKPGDVERRL
SVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQ
KFEACNYPLELYERVRMGPSSSPIPSPSPSPTDSKRCFFGASPGRLHISDFSFLMVLGKG
SFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQL
HSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRD
LKLDNVMLDAEGHIKITDFGMCKENVFPGSTTRTFCGTPDYIAPEIIAYQPYGKSVDWWS
FGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGS
GPDGEPTIRAHGFFRWIDWERLERLEIAPPFRPRPCGRSGENFDKFFTRAAPALTPPDRL
VLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM
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BDBM50136008 |
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n/a |
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Name | BDBM50136008 |
Synonyms: | 12-(3-hydroxypropyl)-9-isopropoxymethyl-6,7,12,13-tetrahydro-5H-indeno[2,1-a]pyrrolo[4,3-c]carbazol-5-one | CHEMBL150894 |
Type | Small organic molecule |
Emp. Form. | C28H28N2O3 |
Mol. Mass. | 440.5335 |
SMILES | CC(C)OCc1ccc2n(CCCO)c3c4Cc5ccccc5-c4c4C(=O)NCc4c3c2c1 |
Structure |
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