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TargetProtein kinase C theta type
LigandBDBM50097494
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1500450 (CHEMBL3587275)
IC50 4.0±n/a nM
Citation Kunikawa, STanaka, AMukoyoshi, KNagashima, STominaga, HChida, NTasaki, MShirai, F Optimization of 2,4-diamino-5-fluoropyrimidine derivatives as protein kinase C theta inhibitors with mitigated time-dependent drug-drug interactions and P-gp liability. Bioorg Med Chem23:3269-77 (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:
BDBM50097494
n/a
NameBDBM50097494
Synonyms:CHEMBL3586035
TypeSmall organic molecule
Emp. Form.C24H34FN9O
Mol. Mass.483.5849
SMILESCOc1cc(Nc2ncc(F)c(NCC3CC(C)(C)N(C)C(C)(C)C3)n2)cc(c1)-n1nnnc1C
Structure
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