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Target
Tyrosine-protein kinase ZAP-70
Ligand
BDBM50151366
Substrate
n/a
Meas. Tech.
ChEMBL_306647 (CHEMBL832984)
IC50
>1000±n/a nM
Citation
 Chen, P; Doweyko, AM; Norris, D; Gu, HH; Spergel, SH; Das, J; Moquin, RV; Lin, J; Wityak, J; Iwanowicz, EJ; McIntyre, KW; Shuster, DJ; Behnia, K; Chong, S; de Fex, H; Pang, S; Pitt, S; Shen, DR; Thrall, S; Stanley, P; Kocy, OR; Witmer, MR; Kanner, SB; Schieven, GL; Barrish, JC Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity. J Med Chem 47:4517-29 (2004) [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:
BDBM50151366
Synonyms:
(2-Chloro-6-methyl-phenyl)-[8-((S)-3-methyl-piperazin-1-yl)-2,5,9,9b-tetraaza-cyclopenta[a]naphthalen-4-yl]-amine | BMS-279700 | CHEMBL189338
Type:
Small organic molecule
Emp. Form.:
C21H22ClN7
Mol. Mass.:
407.899
SMILES:
C[C@H]1CN(CCN1)c1ccc2nc(Nc3c(C)cccc3Cl)c3cncn3c2n1
Structure:
Search PDB for entries with ligand similarity: