Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2166136

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to recombinant MAPKAP-K2 using KKKALSRQLSVAA as substrate after 4 mins by surface plasmon resonance spectroscopic analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

MAP kinase-activated protein kinase 2 (CHEMBL2208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach.
Kosugi T, Mitchell DR, Fujino A, Imai M, Kambe M, Kobayashi S, Makino H, Matsueda Y, Oue Y, Komatsu K, Imaizumi K, Sakai Y, Sugiura S, Takenouchi O, Unoki G, Yamakoshi Y, Cunliffe V, Frearson J, Gordon R, Harris CJ, Kalloo-Hosein H, Le J, Patel G, Simpson DJ, Sherborne B, Thomas PS, Suzuki N, Takimoto-Kamimura M, Kataoka K.
J Med Chem (2012) 55 : 6700 -6715
PubMed 22746295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231206 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231206 IC50 = 5.0 nM 8.30