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Target
Protein kinase C theta type
Ligand
BDBM50240303
Substrate
n/a
Meas. Tech.
ChEMBL_1668070 (CHEMBL4017958)
IC50
6.7±n/a nM
Citation
 Katoh, T; Tomata, Y; Setoh, M; Sasaki, S; Takai, T; Yoshitomi, Y; Yukawa, T; Nakagawa, H; Fukumoto, S; Tsukamoto, T; Nakada, Y Practical application of 3-substituted-2,6-difluoropyridines in drug discovery: Facile synthesis of novel protein kinase C theta inhibitors. Bioorg Med Chem Lett 27:2497-2501 (2017) [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:
BDBM50240303
Synonyms:
CHEMBL4093591
Type:
Small organic molecule
Emp. Form.:
C15H14ClN5O2
Mol. Mass.:
331.757
SMILES:
CN1CCCOc2ccnc3[nH]c(=O)n(-c4nc1ccc4Cl)c23
Structure:
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