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Target
Protein kinase C theta type
Ligand
BDBM25559
Substrate
PKC Peptide Substrate
Meas. Tech.
PKC theta IMAP Kinase Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
2200±400 nM
Citation
 Cole, DC; Asselin, M; Brennan, A; Czerwinski, R; Ellingboe, JW; Fitz, L; Greco, R; Huang, X; Joseph-McCarthy, D; Kelly, MF; Kirisits, M; Lee, J; Li, Y; Morgan, P; Stock, JR; Tsao, DH; Wissner, A; Yang, X; Chaudhary, D Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors. J Med Chem 51:5958-63 (2008) [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:
BDBM25559
Synonyms:
4-arylamino-3-pyridinecarbonitrile, 4q | 5-(3,4-dimethoxyphenyl)-4-(1H-indol-6-ylamino)pyridine-3-carbonitrile | BMCL192461 Compound 1b | CHEMBL492252
Type:
Small organic molecule
Emp. Form.:
C22H18N4O2
Mol. Mass.:
370.4039
SMILES:
COc1ccc(cc1OC)-c1cncc(C#N)c1Nc1ccc2cc[nH]c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PKC Peptide Substrate
Synonyms:
n/a
Type:
Fluorescent peptide
Mol. Mass.:
2051.95
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
FAMRFARKGSLRQKNVH