Reaction Details |
| Report a problem with these data |
Target | Serine/threonine-protein kinase/endoribonuclease IRE1 [547-977] |
---|
Ligand | BDBM192734 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | Kinase Assay |
---|
pH | 7.5±n/a |
---|
IC50 | 3.2e+2± 2e+1 nM |
---|
Comments | extracted |
---|
Citation | Feldman, HC; Tong, M; Wang, L; Meza-Acevedo, R; Gobillot, TA; Lebedev, I; Gliedt, MJ; Hari, SB; Mitra, AK; Backes, BJ; Papa, FR; Seeliger, MA; Maly, DJ Structural and Functional Analysis of the Allosteric Inhibition of IRE1a with ATP-Competitive Ligands. ACS Chem Biol11:2195-205 (2016) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Serine/threonine-protein kinase/endoribonuclease IRE1 [547-977] |
---|
Name: | Serine/threonine-protein kinase/endoribonuclease IRE1 [547-977] |
Synonyms: | ERN1 | ERN1_HUMAN | IRE1 | IRE1α |
Type: | Protein |
Mol. Mass.: | 49232.75 |
Organism: | Homo sapiens (Human) |
Description: | Cytosolic kinase and RNase domains of human IRE1α (residues 547-977) in SF9 insect cells |
Residue: | 431 |
Sequence: | GSSPSLEQDDGDEETSVVIVGKISFCPKDVLGHGAEGTIVYRGMFDNRDVAVKRILPECF
SFADREVQLLRESDEHPNVIRYFCTEKDRQFQYIAIELCAATLQEYVEQKDFAHLGLEPI
TLLQQTTSGLAHLHSLNIVHRDLKPHNILISMPNAHGKIKAMISDFGLCKKLAVGRHSFS
RRSGVPGTEGWIAPEMLSEDCKENPTYTVDIFSAGCVFYYVISEGSHPFGKSLQRQANIL
LGACSLDCLHPEKHEDVIARELIEKMIAMDPQKRPSAKHVLKHPFFWSLEKQLQFFQDVS
DRIEKESLDGPIVKQLERGGRAVVKMDWRENITVPLQTDLRKFRTYKGGSVRDLLRAMRN
KKHHYRELPAEVRETLGSLPDDFVCYFTSRFPHLLAHTYRAMELCSHERLFQPYYFHEPP
EPQPPVTPDAL
|
|
|
BDBM192734 |
---|
n/a |
---|
Name | BDBM192734 |
Synonyms: | KIRA analog, 16 |
Type | Small organic molecule |
Emp. Form. | C28H26N6OS |
Mol. Mass. | 494.611 |
SMILES | CSc1cccc(NC(=O)Nc2ccc(-c3nc(n4ccnc(N)c34)C3(C)CC3)c3ccccc23)c1 |
Structure |
|