Reaction Details |
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Target | Protein kinase C theta type |
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Ligand | BDBM25558 |
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Substrate/Competitor | PKC Peptide Substrate |
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Meas. Tech. | PKC theta IMAP Kinase Assay |
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pH | 7.2±n/a |
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Temperature | 295.15±n/a K |
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Ki | 79±4 nM |
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IC50 | 70±30 nM |
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Citation | Cole, DC; Asselin, M; Brennan, A; Czerwinski, R; Ellingboe, JW; Fitz, L; Greco, R; Huang, X; Joseph-McCarthy, D; Kelly, MF; Kirisits, M; Lee, J; Li, Y; Morgan, P; Stock, JR; Tsao, DH; Wissner, A; Yang, X; Chaudhary, D Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors. J Med Chem51:5958-63 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Protein kinase C theta type |
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Name: | Protein kinase C theta type |
Synonyms: | KPCT_HUMAN | PRKCQ | PRKCT | Protein kinase C theta | Protein kinase C theta type (PRKCQ) | Protein kinase C, PKC; classical/novel | nPKC-theta |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 81878.04 |
Organism: | Homo sapiens (Human) |
Description: | Full-length human PKC theta (Panvera Catalog No. P2996). |
Residue: | 706 |
Sequence: | MSPFLRIGLSNFDCGSCQSCQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTF
DAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGKTEIWLELKPQGRMLMNAR
YFLEMSDTKDMNEFETEGFFALHQRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFV
WGLNKQGYQCRQCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYK
SPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQ
ARCLRDTEQIFREGPVEIGLPCSIKNEARPPCLPTPGKREPQGISWESPLDEVDKMCHLP
EPELNKERPSLQIKLKIEDFILHKMLGKGSFGKVFLAEFKKTNQFFAIKALKKDVVLMDD
DVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSR
ATFYAAEIILGLQFLHSKGIVYRDLKLDNILLDKDGHIKIADFGMCKENMLGDAKTNTFC
GTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPR
WLEKEAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPFD
CSNFDKEFLNEKPRLSFADRALINSMDQNMFRNFSFMNPGMERLIS
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BDBM25558 |
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PKC Peptide Substrate |
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Name: | PKC Peptide Substrate |
Synonyms: | n/a |
Type: | Fluorescent peptide |
Mol. Mass.: | 2051.95 |
Organism: | n/a |
Description: | n/a |
Residue: | 17 |
Sequence: | |