Reaction Details |
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Target | Protein kinase C theta type |
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Ligand | BDBM50525583 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1897549 (CHEMBL4399584) |
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Ki | 6.0±n/a nM |
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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 Lett10:1134-1139 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C theta type |
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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: | MSPFLRIGLSNFDCGSCQSCQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTF
DAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGKTEIWLELKPQGRMLMNAR
YFLEMSDTKDMNEFETEGFFALHQRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFV
WGLNKQGYQCRQCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYK
SPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQ
ARCLRDTEQIFREGPVEIGLPCSIKNEARPPCLPTPGKREPQGISWESPLDEVDKMCHLP
EPELNKERPSLQIKLKIEDFILHKMLGKGSFGKVFLAEFKKTNQFFAIKALKKDVVLMDD
DVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSR
ATFYAAEIILGLQFLHSKGIVYRDLKLDNILLDKDGHIKIADFGMCKENMLGDAKTNTFC
GTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPR
WLEKEAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPFD
CSNFDKEFLNEKPRLSFADRALINSMDQNMFRNFSFMNPGMERLIS
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BDBM50525583 |
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n/a |
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Name | BDBM50525583 |
Synonyms: | CHEMBL4461649 |
Type | Small organic molecule |
Emp. Form. | C17H15F3N4O |
Mol. Mass. | 348.3224 |
SMILES | NCC1(COC1)c1cccc(c1)-c1ccnc2[nH]nc(c12)C(F)(F)F |
Structure |
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