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Assay Detail

CHEMBL2089873

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

Binding
Inhibition of JNK1-mediated ATF2 phosphorylation after 1 hr by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 8 (CHEMBL2276)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.
Kusakabe K, Ide N, Daigo Y, Itoh T, Higashino K, Okano Y, Tadano G, Tachibana Y, Sato Y, Inoue M, Wada T, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Tagashira S, Kido Y, Sakamoto S, Yasuo K, Maeda M, Yamamoto T, Higaki M, Endoh T, Ueda K, Shiota T, Murai H, Nakamura Y.
ACS Med Chem Lett (2012) 3 : 560 -564
PubMed 24900510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.79 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424872 1 8.33
CHEMBL2089254 1 6.72
CHEMBL2089255 1 6.64
CHEMBL210861 1 6.58
CHEMBL211195 1 6.46
CHEMBL2089253 1 5.99
CHEMBL2089252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424872 IC50 = 4.7 nM 8.33
CHEMBL2089254 IC50 = 190.0 nM 6.72
CHEMBL2089255 IC50 = 231.0 nM 6.64
CHEMBL210861 IC50 = 260.0 nM 6.58
CHEMBL211195 IC50 = 350.0 nM 6.46
CHEMBL2089253 IC50 = 1035.0 nM 5.99
CHEMBL2089252 IC50 > 100000.0 nM -