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Assay Detail

CHEMBL2437702

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

Binding
Inhibition of MLK3 in mouse BV2 cells assessed as inhibition of LPS-induced TNFalpha release after 8 hrs by ELISA
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BV-2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 11 (CHEMBL2434817)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O, Marker DF, Dewhurst S, Gelbard HA.
J Med Chem (2013) 56 : 8032 -8048
PubMed 24044867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.02 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2436982 1 6.92
CHEMBL2436981 1 6.37
CHEMBL2436978 1 6.34
CHEMBL2436983 1 6.29
CHEMBL2436976 1 6.00
CHEMBL2436980 1 5.57
CHEMBL2436979 1 4.63
CHEMBL2436977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2436982 IC50 = 120.0 nM 6.92
CHEMBL2436981 IC50 = 430.0 nM 6.37
CHEMBL2436978 IC50 = 460.0 nM 6.34
CHEMBL2436983 IC50 = 510.0 nM 6.29
CHEMBL2436976 IC50 = 990.0 nM 6.00
CHEMBL2436980 IC50 = 2700.0 nM 5.57
CHEMBL2436979 IC50 = 23600.0 nM 4.63
CHEMBL2436977 IC50 - -