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Target
Tyrosine-protein kinase ZAP-70
Ligand
BDBM5058
Substrate
ZAP-70 SH2 Binding Substrate
Meas. Tech.
Competitive Binding Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
36000±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:
BDBM5058
Synonyms:
1,2,4-Oxadiazole Analogue 4c | 4-[(2S)-2-{[(1S)-3-carbamoyl-1-(3-{[4-(propan-2-yl)phenyl]methyl}-1,2,4-oxadiazol-5-yl)propyl]carbamoyl}-2-acetamidoethyl]phenoxyphosphonic acid
Type:
Small organic molecule
Emp. Form.:
C27H34N5O8P
Mol. Mass.:
587.5613
SMILES:
CC(C)c1ccc(Cc2noc(n2)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccc(OP(O)(O)=O)cc2)NC(C)=O)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