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Target
Protein kinase C theta type
Ligand
BDBM50258385
Substrate
n/a
Meas. Tech.
ChEMBL_523117 (CHEMBL1007475)
IC50
55±n/a nM
Citation
 Boschelli, DH; Wang, D; Prashad, AS; Subrath, J; Wu, B; Niu, C; Lee, J; Yang, X; Brennan, A; Chaudhary, D Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors. Bioorg Med Chem Lett 19:3623-6 (2009) [PubMed]  Article 
Target
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:
MSPFLRIGLSNFDCGSCQSCQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTFDAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGKTEIWLELKPQGRMLMNARYFLEMSDTKDMNEFETEGFFALHQRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFVWGLNKQGYQCRQCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYKSPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQARCLRDTEQIFREGPVEIGLPCSIKNEARPPCLPTPGKREPQGISWESPLDEVDKMCHLPEPELNKERPSLQIKLKIEDFILHKMLGKGSFGKVFLAEFKKTNQFFAIKALKKDVVLMDDDVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSRATFYAAEIILGLQFLHSKGIVYRDLKLDNILLDKDGHIKIADFGMCKENMLGDAKTNTFCGTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPRWLEKEAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPFDCSNFDKEFLNEKPRLSFADRALINSMDQNMFRNFSFMNPGMERLIS
  
Inhibitor
Name:
BDBM50258385
Synonyms:
5-(3,4-dimethoxyphenyl)-4-(4-ethyl-1H-indol-5-ylamino)nicotinonitrile | CHEMBL494000
Type:
Small organic molecule
Emp. Form.:
C24H22N4O2
Mol. Mass.:
398.4571
SMILES:
CCc1c(Nc2c(cncc2-c2ccc(OC)c(OC)c2)C#N)ccc2[nH]ccc12
Structure:
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