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Target
Protein kinase C theta type
Ligand
BDBM29825
Substrate
PKC Peptide Substrate
Meas. Tech.
PKC theta IMAP Kinase Assay
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
190±n/a nM
Citation
Dushin, RG; Nittoli, T; Ingalls, C; Boschelli, DH; Cole, DC; Wissner, A; Lee, J; Yang, X; Morgan, P; Brennan, A; Chaudhary, D Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles. Bioorg Med Chem Lett 19:2461-3 (2009) [PubMed] Article
More Info.:
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:
BDBM29825
Synonyms:
4-indolylamino-5-phenyl-3-pyridinecarbonitrile, 12e
Type:
Small organic molecule
Emp. Form.:
C26H25N5O
Mol. Mass.:
423.5096
SMILES:
N#Cc1cncc(-c2cccc(OCCN3CCCC3)c2)c1Nc1ccc2[nH]ccc2c1
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