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Target
Tyrosine-protein kinase ZAP-70
Ligand
BDBM5089
Substrate
ZAP-70 SH2 Binding Substrate
Meas. Tech.
Competitive Binding Assay
IC50
6000±n/a nM
Citation
 Vu, CB; Corpuz, EG; Merry, TJ; Pradeepan, SG; Bartlett, C; Bohacek, RS; Botfield, MC; Eyermann, CJ; Lynch, BA; MacNeil, IA; Ram, MK; van Schravendijk, MR; Violette, S; Sawyer, TK Discovery of potent and selective SH2 inhibitors of the tyrosine kinase ZAP-70. J Med Chem 42:4088-98 (1999) [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:
BDBM5089
Synonyms:
1,2,4-Oxadiazole Analogue 14d | 4-[(2S)-2-[1-(4-methoxyphenyl)acetamido]-2-{[(1S)-1-(3-{[4-(trifluoromethyl)phenyl]methyl}-1,2,4-oxadiazol-5-yl)ethyl]carbamoyl}ethyl]phenoxyphosphonic acid
Type:
Small organic molecule
Emp. Form.:
C30H30F3N4O8P
Mol. Mass.:
662.5502
SMILES:
COc1ccc(CC(=O)N[C@@H](Cc2ccc(OP(O)(O)=O)cc2)C(=O)N[C@@H](C)c2nc(Cc3ccc(cc3)C(F)(F)F)no2)cc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ZAP-70 SH2 Binding Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2801.56
Organism:
n/a
Description:
n/a
Residue:
23
Sequence:
FLRGPYNELNLGRREEPYDVLNH