Reaction Details |
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Target | Protein kinase C alpha/beta/delta/epsilon/eta/gamma/theta/zeta type |
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Ligand | BDBM2579 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_162388 (CHEMBL767476) |
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IC50 | 9±n/a nM |
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Citation | Kleinschroth, J; Hartenstein, J; Rudolph, C; Schächtele, C Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C Bioorg Med Chem Lett3:1959-1964 (1993) Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C alpha/beta/delta/epsilon/eta/gamma/theta/zeta type |
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Name: | Protein kinase C alpha/beta/delta/epsilon/eta/gamma/theta/zeta type |
Synonyms: | Protein kinase C (PKC) |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 162388 |
Components: | This complex has 8 components. |
Component 1 |
Name: | Protein kinase C delta type |
Synonyms: | KPCD_RAT | Pkcd | Prkcd | Protein kinase C delta type | Protein kinase C delta type catalytic subunit | Protein kinase C delta type regulatory subunit | SDK1 | Sphingosine-dependent protein kinase-1 | nPKC-delta |
Type: | PROTEIN |
Mol. Mass.: | 77531.57 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_104731 |
Residue: | 673 |
Sequence: | MAPFLRISFNSYELGSLQAEDDASQPFCAVKMKEALTTDRGKTLVQKKPTMYPEWKSTFD
AHIYEGRVIQIVLMRAAEDPMSEVTVGVSVLAERCKKNNGKAEFWLDLQPQAKVLMCVQY
FLEDGDCKQSMRSEEEAMFPTMNRRGAIKQAKIHYIKNHEFIATFFGQPTFCSVCKEFVW
GLNKQGYKCRQCNAAIHKKCIDKIIGRCTGTATNSRDTIFQKERFNIDMPHRFKVYNYMS
PTFCDHCGTLLWGLVKQGLKCEDCGMNVHHKCREKVANLCGINQKLLAEALNQVTQKASR
KPETPETVGIYQGFEKKTAVSGNDIPDNNGTYGKIWEGSNRCRLENFTFQKVLGKGSFGK
VLLAELKGKERYFAIKYLKKDVVLIDDDVECTMVEKRVLALAWENPFLTHLICTFQTKDH
LFFVMEFLNGGDLMFHIQDKGRFELYRATFYAAEIICGLQFLHGKGIIYRDLKLDNVMLD
KDGHIKIADFGMCKENIFGENRASTFCGTPDYIAPEILQGLKYSFSVDWWSFGVLLYEML
IGQSPFHGDDEDELFESIRVDTPHYPRWITKESKDIMEKLFERDPAKRLGVTGNIRLHPF
FKTINWNLLEKRKVEPPFKPKVKSPSDYSNFDPEFLNEKPQLSFSDKNLIDSMDQTAFKG
FSFVNPKYEQFLE
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Component 2 |
Name: | Protein kinase C eta type |
Synonyms: | KPCL_RAT | PKC-L | Pkch | Prkch | Protein kinase C eta type | nPKC-eta |
Type: | PROTEIN |
Mol. Mass.: | 77961.39 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_104731 |
Residue: | 683 |
Sequence: | MSSGTMKFNGYLRVRIGEAVGLQPTRWSLRHSLFKKGHQLLDPYLTVSVDQVRVGQTSTK
QKTNKPTYNEEFCTNVSDGGHLELAVFHETPLGYDHFVANCTLQFQELLRTAGTSDTFEG
WVDLEPEGKVFVVITLTGSFTEATLQRDRIFKHFTRKRQRAMRRRVHQVNGHKFMATYLR
QPTYCSHCREFIWGVFGKQGYQCQVCTCVVHKRCHHLIVTACTCQNNINKVDAKIAEQRF
GINIPHKFNVHNYKVPTFCDHCGSLLWGIMRQGLQCKICKMNVHIRCQANVAPNCGVNAV
ELAKTLAGMGLQPGNISPTSKLISRSTLRRQGKEGSKEGNGIGVNSSSRFGIDNFEFIRV
LGKGSFGKVMLARIKETGELYAVKVLKKDVILQDDDVECTMTEKRILSLARNHPFLTQLF
CCFQTPDRLFFVMEFVNGGDLMFHIQKSRRFDEARARFYAAEIISALMFLHEKGIIYRDL
KLDNVLLDHEGHCKLADFGMCKEGICNGVTTATFCGTPDYIAPEILQEMLYGPAVDWWAM
GVLLYEMLCGHAPFEAENEDDLFEAILNDEVVYPTWLHEDATGILKSFMTKNPTMRLGSL
TQGGEHEILRHPFFKEIDWVQLNHRQLEPPFRPRIKSREDVSNFDPDFIKEEPVLTPIDE
GHLPMINQDEFRNFSYVSPELQP
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Component 3 |
Name: | Protein kinase C theta type |
Synonyms: | KPCT_RAT | Pkcq | Prkcq | Protein kinase C theta type | nPKC-theta |
Type: | PROTEIN |
Mol. Mass.: | 81765.17 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_104731 |
Residue: | 707 |
Sequence: | MSPFLRIGLSNFDCGTCQACQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTF
DAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGRTEIWLELKPQGRMLMNAR
YFLEMSDTKDMSEFENEGFFALHHRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFV
WGLNKQGYQCRRCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYK
SPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQ
ARTLRDSEHIFREGPIEISFPRSIKSETRPPCVPTPGKSEPQGICWESPLDGADKTAQPP
EPEVNLQRASLQLKLKIDDFILHKMLGKGSFGKVFLAEFKRTKQFFAIKALKKDVVLMDD
DVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSR
ATFYAAEVILGLQFLHSKGIVYRDLKLDNILLDRDGHIKIADFGMCKENMLGDAKTNTFC
GTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPR
WLEREAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPYD
CSNFDKEFLSEKPRLSFADRALINSMDQNMFSNFSFINPGMETLICS
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Component 4 |
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 5 |
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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Component 6 |
Name: | Protein kinase C zeta type |
Synonyms: | KPCZ_RAT | Pkcz | Prkcz | Protein kinase C (PKC) | Protein kinase C zeta type | nPKC-zeta |
Type: | PROTEIN |
Mol. Mass.: | 67722.31 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_104731 |
Residue: | 592 |
Sequence: | MPSRTDPKMDRSGGRVRLKAHYGGDILITSVDPTTTFQDLCEEVRDMCGLHQQHPLTLKW
VDSEGDPCTVSSQMELEEAFRLACQGRDEVLIIHVFPSIPEQPGMPCPGEDKSIYRRGAR
RWRKLYRANGHLFQAKRFNRRAYCGQCSERIWGLARQGYRCINCKLLVHKRCHVLVPLTC
RRHMDSVMPSQEPPVDDKNDGVDLPSEETDGIAYISSSRKHDNIKDDSEDLKPVIDGVDG
IKISQGLGLQDFDLIRVIGRGSYAKVLLVRLKKNDQIYAMKVVKKELVHDDEDIDWVQTE
KHVFEQASSNPFLVGLHSCFQTTSRLFLVIEYVNGGDLMFHMQRQRKLPEEHARFYAAEI
CIALNFLHERGIIYRDLKLDNVLLDADGHIKLTDYGMCKEGLGPGDTTSTFCGTPNYIAP
EILRGEEYGFSVDWWALGVLMFEMMAGRSPFDIITDNPDMNTEDYLFQVILEKPIRIPRF
LSVKASHVLKGFLNKDPKERLGCRPQTGFSDIKSHAFFRSIDWDLLEKKQTLPPFQPQIT
DDYGLDNFDTQFTSEPVQLTPDDEDVIKRIDQSEFEGFEYINPLLLSAEESV
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Component 7 |
Name: | Protein kinase C epsilon type |
Synonyms: | KPCE_RAT | Pkce | Prkce | Protein kinase C (PKC) | Protein kinase C epsilon | Protein kinase C epsilon type | nPKC-epsilon |
Type: | PROTEIN |
Mol. Mass.: | 83483.06 |
Organism: | Rattus norvegicus |
Description: | ChEMBL_160964 |
Residue: | 737 |
Sequence: | MVVFNGLLKIKICEAVSLKPTAWSLRHAVGPRPQTFLLDPYIALNVDDSRIGQTATKQKT
NSPAWHDEFVTDVCNGRKIELAVFHDAPIGYDDFVANCTIQFEELLQNGSRHFEDWIDLE
PEGKVYVIIDLSGSSGEAPKDNEERVFRERMRPRKRQGAVRRRVHQVNGHKFMATYLRQP
TYCSHCRDFIWGVIGKQGYQCQVCTCVVHKRCHELIITKCAGLKKQETPDEVGSQRFSVN
MPHKFGIHNYKVPTFCDHCGSLLWGLLRQGLQCKVCKMNVHRRCETNVAPNCGVDARGIA
KVLADLGVTPDKITNSGQRRKKLAAGAESPQPASGNSPSEDDRSKSAPTSPCDQELKELE
NNIRKALSFDNRGEEHRASSSTDGQLASPGENGEVRQGQAKRLGLDEFNFIKVLGKGSFG
KVMLAELKGKDEVYAVKVLKKDVILQDDDVDCTMTEKRILALARKHPYLTQLYCCFQTKD
RLFFVMEYVNGGDLMFQIQRSRKFDEPRSGFYAAEVTSALMFLHQHGVIYRDLKLDNILL
DAEGHSKLADFGMCKEGILNGVTTTTFCGTPDYIAPEILQELEYGPSVDWWALGVLMYEM
MAGQPPFEADNEDDLFESILHDDVLYPVWLSKEAVSILKAFMTKNPHKRLGCVAAQNGED
AIKQHPFFKEIDWVLLEQKKMKPPFKPRIKTKRDVNNFDQDFTREEPILTLVDEAIVKQI
NQEEFKGFSYFGEDLMP
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Component 8 |
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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BDBM2579 |
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n/a |
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Name | BDBM2579 |
Synonyms: | (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine |
Type | Small organic molecule |
Emp. Form. | C28H26N4O3 |
Mol. Mass. | 466.531 |
SMILES | CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| |
Structure |
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