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Target
Protein kinase C theta type
Ligand
BDBM50525597
Substrate
n/a
Meas. Tech.
ChEMBL_1897549 (CHEMBL4399584)
Ki
8.0±n/a nM
Citation
 Collier, PN; Twin, HC; Knegtel, RMA; Boyall, D; Brenchley, G; Davis, CJ; Keily, S; Mak, C; Miller, A; Pierard, F; Settimo, L; Bolton, CM; Chiu, P; Curnock, A; Doyle, E; Tanner, AJ; Jimenez, JM Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis. ACS Med Chem Lett 10:1134-1139 (2019) [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:
BDBM50525597
Synonyms:
CHEMBL4587816
Type:
Small organic molecule
Emp. Form.:
C18H17F3N4O
Mol. Mass.:
362.349
SMILES:
Cc1cc(cc(c1)C1(CN)COC1)-c1ccnc2[nH]nc(c12)C(F)(F)F
Structure:
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