Reaction Details |
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Target | Protein kinase C theta type |
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Ligand | BDBM50097494 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1500450 (CHEMBL3587275) |
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IC50 | 4.0±n/a nM |
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Citation | Kunikawa, S; Tanaka, A; Mukoyoshi, K; Nagashima, S; Tominaga, H; Chida, N; Tasaki, M; Shirai, F Optimization of 2,4-diamino-5-fluoropyrimidine derivatives as protein kinase C theta inhibitors with mitigated time-dependent drug-drug interactions and P-gp liability. Bioorg Med Chem23:3269-77 (2015) [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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BDBM50097494 |
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n/a |
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Name | BDBM50097494 |
Synonyms: | CHEMBL3586035 |
Type | Small organic molecule |
Emp. Form. | C24H34FN9O |
Mol. Mass. | 483.5849 |
SMILES | COc1cc(Nc2ncc(F)c(NCC3CC(C)(C)N(C)C(C)(C)C3)n2)cc(c1)-n1nnnc1C |
Structure |
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