Reaction Details |
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Target | Protein kinase C theta type |
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Ligand | BDBM50028442 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1436875 (CHEMBL3387797) |
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IC50 | 4.0±n/a nM |
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Citation | George, DM; Breinlinger, EC; Argiriadi, MA; Zhang, Y; Wang, J; Bansal-Pakala, P; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Rundell, L; Schwartz, A; Sun, J; Edmunds, JJ Optimized protein kinase C¿ (PKC¿) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis. J Med Chem58:333-46 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50028442 |
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n/a |
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Name | BDBM50028442 |
Synonyms: | CHEMBL3355118 |
Type | Small organic molecule |
Emp. Form. | C23H26FN5O2 |
Mol. Mass. | 423.4832 |
SMILES | C[C@H]1N2C(COc3cc(c(cc23)N(C)C2(C)CN(C)C2)-c2ccccc2F)=NNC1=O |r,c:30| |
Structure |
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