Reaction Details
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Target
Mitogen-activated protein kinase kinase kinase kinase 2
Ligand
BDBM38325
Substrate
n/a
Meas. Tech.
Dose Response of SAR compounds via Multiplex HTS Assay for Inhibitors of MEK Kinase PB1 Domains, specifically MEK5 binding to MEK Kinase 2 Wildtype
EC50
>30000±n/a nM
Citation
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More Info.:
Target
Name:
Mitogen-activated protein kinase kinase kinase kinase 2
Synonyms:
2.7.11.1 | B lymphocyte serine/threonine-protein kinase | GC kinase | GCK | Germinal center kinase | M4K2_HUMAN | MAP4K2 | MAPK/ERK kinase kinase kinase 2 | MEK kinase kinase 2 | MEKKK 2 | RAB8IP | Rab8-interacting protein
Type:
n/a
Mol. Mass.:
91551.35
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
820
Sequence:
MALLRDVSLQDPRDRFELLQRVGAGTYGDVYKARDTVTSELAAVKIVKLDPGDDISSLQQEITILRECRHPNVVAYIGSYLRNDRLWICMEFCGGGSLQEIYHATGPLEERQIAYVCREALKGLHHLHSQGKIHRDIKGANLLLTLQGDVKLADFGVSGELTASVAKRRSFIGTPYWMAPEVAAVERKGGYNELCDVWALGITAIELGELQPPLFHLHPMRALMLMSKSSFQPPKLRDKTRWTQNFHHFLKLALTKNPKKRPTAEKLLQHPFTTQQLPRALLTQLLDKASDPHLGTPSPEDCELETYDMFPDTIHSRGQHGPAERTPSEIQFHQVKFGAPRRKETDPLNEPWEEEWTLLGKEELSGSLLQSVQEALEERSLTIRSASEFQELDSPDDTMGTIKRAPFLGPLPTDPPAEEPLSSPPGTLPPPPSGPNSSPLLPTAWATMKQREDPERSSCHGLPPTPKVHMGACFSKVFNGCPLRIHAAVTWIHPVTRDQFLVVGAEEGIYTLNLHELHEDTLEKLISHRCSWLYCVNNVLLSLSGKSTHIWAHDLPGLFEQRRLQQQVPLSIPTNRLTQRIIPRRFALSTKIPDTKGCLQCRVVRNPYTGATFLLAALPTSLLLLQWYEPLQKFLLLKNFSSPLPSPAGMLEPLVLDGKELPQVCVGAEGPEGPGCRVLFHVLPLEAGLTPDILIPPEGIPGSAQQVIQVDRDTILVSFERCVRIVNMQGEPTATLAPELTFDFPIETVVCLQDSVLAFWSHGMQGRSLDTNEVTQEITDETRIFRVLGAHRDIILESIPTDNPEAHSNLYILTGHQSTY
Inhibitor
Name:
BDBM38325
Synonyms:
6-(3,4-dimethoxyphenyl)-3-(2-pyridinyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole | 6-(3,4-dimethoxyphenyl)-3-(2-pyridyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole | 6-(3,4-dimethoxyphenyl)-3-pyridin-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole | MLS000081176 | SMR000043689 | cid_662931
Type:
Small organic molecule
Emp. Form.:
C16H13N5O2S
Mol. Mass.:
339.372
SMILES:
COc1ccc(cc1OC)-c1nn2c(nnc2s1)-c1ccccn1