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TargetProtein kinase C theta type
LigandBDBM50028442
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1436875 (CHEMBL3387797)
IC50 4.0±n/a nM
Citation George, DMBreinlinger, ECArgiriadi, MAZhang, YWang, JBansal-Pakala, PDuignan, DBHonore, PLang, QMittelstadt, SRundell, LSchwartz, ASun, JEdmunds, 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
More Info.:Get all data from this article,  Assay Method
 
Protein kinase C theta type
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50028442
n/a
NameBDBM50028442
Synonyms:CHEMBL3355118
TypeSmall organic molecule
Emp. Form.C23H26FN5O2
Mol. Mass.423.4832
SMILESC[C@H]1N2C(COc3cc(c(cc23)N(C)C2(C)CN(C)C2)-c2ccccc2F)=NNC1=O |r,c:30|
Structure
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