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Target
Protein kinase C theta type
Ligand
BDBM50133057
Substrate
n/a
Meas. Tech.
ChEMBL_161442 (CHEMBL772576)
IC50
65±n/a nM
Citation
 Kuo, GH; Prouty, C; DeAngelis, A; Shen, L; O'Neill, DJ; Shah, C; Connolly, PJ; Murray, WV; Conway, BR; Cheung, P; Westover, L; Xu, JZ; Look, RA; Demarest, KT; Emanuel, S; Middleton, SA; Jolliffe, L; Beavers, MP; Chen, X Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. J Med Chem 46:4021-31 (2003) [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:
BDBM50133057
Synonyms:
17,20,23-trioxa-4,14,26-triazahexacyclo[24.6.1.17,14.02,6.08,13.027,32]tetratriaconta-1(33),2(6),7(34),8,10,12,27,29,31-nonaene-3,5-dione | CHEMBL340259 | Indolylylmaleimide 2
Type:
Small organic molecule
Emp. Form.:
C28H27N3O5
Mol. Mass.:
485.5311
SMILES:
O=C1NC(=O)C2=C1c1cn(CCOCCOCCOCCn3cc2c2ccccc32)c2ccccc12 |c:5|
Structure:
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