| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
|---|
| Ligand | BDBM27452 |
|---|
| Substrate/Competitor | I-kappa-B-alpha |
|---|
| Meas. Tech. | IKK Kinase Inhibition Assay |
|---|
| pH | 7.4±n/a |
|---|
| Temperature | 295.15±n/a K |
|---|
| IC50 | 40±n/a nM |
|---|
| Citation |  Bamborough, P; Christopher, JA; Cutler, GJ; Dickson, MC; Mellor, GW; Morey, JV; Patel, CB; Shewchuk, LM 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase. Bioorg Med Chem Lett16:6236-40 (2006) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
|---|
| |
| Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
|---|
| Name: | Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
|---|
| Synonyms: | I kappa-B kinase epsilon | I-kappa-B Kinase 3 (IKK-epsilon) | I-kappa-B kinase epsilon (IKK-E) | I-kappa-B kinase epsilon (IKKE) | IKBKE | IKK-E | IKK-epsilon | IKK-i | IKKE | IKKE_HUMAN | IKKI | Inducible I kappa-B kinase | KIAA0151 | von Hippel-Lindau disease tumor suppressor/Inhibitor of nuclear factor kappa-B kinase subunit epsilon |
|---|
| Type: | Serine/threonine-protein kinase |
|---|
| Mol. Mass.: | 80475.98 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Kinase inhibitory activity was determined using recombinant human IKK-epsilon expressed in baculovirus as a FLAG-tagged fusion protein. |
|---|
| Residue: | 716 |
|---|
| Sequence: | MQSTANYLWHTDDLLGQGATASVYKARNKKSGELVAVKVFNTTSYLRPREVQVREFEVLR
KLNHQNIVKLFAVEETGGSRQKVLVMEYCSSGSLLSVLESPENAFGLPEDEFLVVLRCVV
AGMNHLRENGIVHRDIKPGNIMRLVGEEGQSIYKLTDFGAARELDDDEKFVSVYGTEEYL
HPDMYERAVLRKPQQKAFGVTVDLWSIGVTLYHAATGSLPFIPFGGPRRNKEIMYRITTE
KPAGAIAGAQRRENGPLEWSYTLPITCQLSLGLQSQLVPILANILEVEQAKCWGFDQFFA
ETSDILQRVVVHVFSLSQAVLHHIYIHAHNTIAIFQEAVHKQTSVAPRHQEYLFEGHLCV
LEPSVSAQHIAHTTASSPLTLFSTAIPKGLAFRDPALDVPKFVPKVDLQADYNTAKGVLG
AGYQALRLARALLDGQELMFRGLHWVMEVLQATCRRTLEVARTSLLYLSSSLGTERFSSV
AGTPEIQELKAAAELRSRLRTLAEVLSRCSQNITETQESLSSLNRELVKSRDQVHEDRSI
QQIQCCLDKMNFIYKQFKKSRMRPGLGYNEEQIHKLDKVNFSHLAKRLLQVFQEECVQKY
QASLVTHGKRMRVVHETRNHLRLVGCSVAACNTEAQGVQESLSKLLEELSHQLLQDRAKG
AQASPPPIAPYPSPTRKDLLLHMQELCEGMKLLASDLLDNNRIIERLNRVPAPPDV
|
|
|
|---|
| BDBM27452 |
|---|
| I-kappa-B-alpha |
|---|
| Name: | NF-kappa-B inhibitor alpha |
|---|
| Synonyms: | I-kappa-B-alpha | IKBA | IKBA_HUMAN | MAD3 | NF-kappa-B inhibitor alpha | NFKBI | NFKBIA |
|---|
| Type: | GST fusion protein |
|---|
| Mol. Mass.: | 35584.84 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | It was produced in E. coli as GST-tagged fusion protein (Santa Cruz Biotechnology). |
|---|
| Residue: | 317 |
|---|
| Sequence: | MFQAAERPQEWAMEGPRDGLKKERLLDDRHDSGLDSMKDEEYEQMVKELQEIRLEPQEVP
RGSEPWKQQLTEDGDSFLHLAIIHEEKALTMEVIRQVKGDLAFLNFQNNLQQTPLHLAVI
TNQPEIAEALLGAGCDPELRDFRGNTPLHLACEQGCLASVGVLTQSCTTPHLHSILKATN
YNGHTCLHLASIHGYLGIVELLVSLGADVNAQEPCNGRTALHLAVDLQNPDLVSLLLKCG
ADVNRVTYQGYSPYQLTWGRPSTRIQQQLGQLTLENLQMLPESEDEESYDTESEFTEFTE
DELPYDDCVFGGQRLTL
|
|
|
|---|
Search and Browse
