Reaction Details |
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Target | Protein kinase C theta type |
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Ligand | BDBM50028445 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1454725 (CHEMBL3362644) |
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IC50 | 23±n/a nM |
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Citation | George, DM; Breinlinger, EC; Friedman, M; Zhang, Y; Wang, J; Argiriadi, M; Bansal-Pakala, P; Barth, M; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Potin, D; Rundell, L; Edmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (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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BDBM50028445 |
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n/a |
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Name | BDBM50028445 |
Synonyms: | CHEMBL3355112 |
Type | Small organic molecule |
Emp. Form. | C16H18F3N5O2 |
Mol. Mass. | 369.3416 |
SMILES | C[C@H]1N2C(COc3cc(c(NC4(C)CNC4)cc23)C(F)(F)F)=NNC1=O |r,c:24| |
Structure |
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