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Target
Tyrosine-protein kinase ZAP-70
Ligand
BDBM50249539
Substrate
n/a
Meas. Tech.
ChEMBL_537398 (CHEMBL992588)
IC50
330±n/a nM
Citation
 Hirabayashi, A; Mukaiyama, H; Kobayashi, H; Shiohara, H; Nakayama, S; Ozawa, M; Tsuji, E; Miyazawa, K; Misawa, K; Ohnota, H; Isaji, M Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors. Bioorg Med Chem 16:9247-60 (2008) [PubMed]  Article
Target
Name:
Tyrosine-protein kinase ZAP-70
Synonyms:
70 kDa zeta-associated protein | SRK | Syk-related tyrosine kinase | Tyrosine Kinase ZAP-70 | Tyrosine-protein kinase ZAP-70 | Tyrosine-protein kinase ZAP-70 (Syk) | Tyrosine-protein kinase ZAP-70 (ZAP70) | Tyrosine-protein kinase ZAP70 | ZAP70 | ZAP70_HUMAN | Zeta-chain (TCR) associated protein kinase 70kDa
Type:
Enzyme
Mol. Mass.:
69881.61
Organism:
Homo sapiens (Human)
Description:
ZAP-70 SH2 domain was expressed and purified from E. coli using O-phospho-L-tyrosine-agarose column.
Residue:
619
Sequence:
MPDPAAHLPFFYGSISRAEAEEHLKLAGMADGLFLLRQCLRSLGGYVLSLVHDVRFHHFPIERQLNGTYAIAGGKAHCGPAELCEFYSRDPDGLPCNLRKPCNRPSGLEPQPGVFDCLRDAMVRDYVRQTWKLEGEALEQAIISQAPQVEKLIATTAHERMPWYHSSLTREEAERKLYSGAQTDGKFLLRPRKEQGTYALSLIYGKTVYHYLISQDKAGKYCIPEGTKFDTLWQLVEYLKLKADGLIYCLKEACPNSSASNASGAAAPTLPAHPSTLTHPQRRIDTLNSDGYTPEPARITSPDKPRPMPMDTSVYESPYSDPEELKDKKLFLKRDNLLIADIELGCGNFGSVRQGVYRMRKKQIDVAIKVLKQGTEKADTEEMMREAQIMHQLDNPYIVRLIGVCQAEALMLVMEMAGGGPLHKFLVGKREEIPVSNVAELLHQVSMGMKYLEEKNFVHRDLAARNVLLVNRHYAKISDFGLSKALGADDSYYTARSAGKWPLKWYAPECINFRKFSSRSDVWSYGVTMWEALSYGQKPYKKMKGPEVMAFIEQGKRMECPPECPPELYALMSDCWIYKWEDRPDFLTVEQRMRACYYSLASKVEGPPGSTQKAEAACA
  
Inhibitor
Name:
BDBM50249539
Synonyms:
5-((1S,2R)-2-aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-[1,2,4]triazolo[1,5-c]pyrimidine-8-carboxamide | 5-((1S,2R)-2-aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-[1,2,4]triazolo[1,5-f]pyrimidine-8-carboxamide | CHEMBL475575 | cis-5-(2-Aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-1,2,4-triazolo[1,5-c]pyrimidine-8-carboxamide
Type:
Small organic molecule
Emp. Form.:
C20H26N8O3
Mol. Mass.:
426.4722
SMILES:
COc1cc(Nc2nc(N[C@H]3CCCC[C@H]3N)n3ncnc3c2C(N)=O)cc(OC)c1 |r|
Structure:
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