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TargetProtein kinase C theta type
LigandBDBM50049437
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1454725 (CHEMBL3362644)
IC50 49±n/a nM
Citation George, DMBreinlinger, ECFriedman, MZhang, YWang, JArgiriadi, MBansal-Pakala, PBarth, MDuignan, DBHonore, PLang, QMittelstadt, SPotin, DRundell, LEdmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (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:
BDBM50049437
n/a
NameBDBM50049437
Synonyms:CHEMBL3356474
TypeSmall organic molecule
Emp. Form.C15H16F3N5O2
Mol. Mass.355.315
SMILESC[C@H]1N2C(COc3cc(c(NC4CNC4)cc23)C(F)(F)F)=NNC1=O |r,c:23|
Structure
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