Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase ZAP-70
Ligand
BDBM26410
Substrate
ZAP-70 Peptide Substrate
Meas. Tech.
Intracellular ZAP-70 Kinase Inhibition Assay
pH
7.6±n/a
Temperature
303.15±n/a K
IC50
220±n/a nM
Citation
 Hirabayashi, A; Mukaiyama, H; Kobayashi, H; Shiohara, H; Nakayama, S; Ozawa, M; Miyazawa, K; Misawa, K; Ohnota, H; Isaji, M Structure-activity relationship studies of 5-benzylaminoimidazo[1,2-c]pyrimidine-8-carboxamide derivatives as potent, highly selective ZAP-70 kinase inhibitors. Bioorg Med Chem 17:284-94 (2009) [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:
BDBM26410
Synonyms:
7-[(3,5-dimethoxyphenyl)amino]-5-{[(4-fluorophenyl)methyl]amino}imidazo[1,2-a]pyrimidine-8-carboxamide | imidazo[1,2-c]pyrimidine-8-carboxamide, 10i
Type:
Small organic molecule
Emp. Form.:
C22H21FN6O3
Mol. Mass.:
436.4389
SMILES:
COc1cc(Nc2nc(NCc3ccc(F)cc3)n3ccnc3c2C(N)=O)cc(OC)c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
ZAP-70 Peptide Substrate
Synonyms:
Syk Peptide Substrate
Type:
Peptide
Mol. Mass.:
1797.98
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
AEEEIYGEFEAKKKK