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Assay Detail

CHEMBL5046418

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

Binding
Inhibition of MAPK8 (unknown origin) incubated for 1 hr by qPCR analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of New Imidazo[2,1-<i>b</i>]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising <i>In Vitro</i> and <i>In Vivo</i> Anti-melanoma Activity.
Abdel-Maksoud MS, El-Gamal MI, Lee BS, Gamal El-Din MM, Jeon HR, Kwon D, Ammar UM, Mersal KI, Ali EMH, Lee KT, Yoo KH, Han DK, Lee JK, Kim G, Choi HS, Kwon YJ, Lee KH, Oh CH.
J Med Chem (2021) 64 : 6877 -6901
PubMed 33999621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.09 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5081210 1 6.44
CHEMBL5073858 1 6.38
CHEMBL5087577 1 6.04
CHEMBL5083036 1 5.87
CHEMBL5086749 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5081210 IC50 = 360.0 nM 6.44
CHEMBL5073858 IC50 = 420.0 nM 6.38
CHEMBL5087577 IC50 = 910.0 nM 6.04
CHEMBL5083036 IC50 = 1350.0 nM 5.87
CHEMBL5086749 IC50 = 1870.0 nM 5.73