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Assay Detail

CHEMBL732489

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

Binding
Inhibition of Mixed lineage kinase 2(MLK2)
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 Expert

Target

Mitogen-activated protein kinase kinase kinase 10 (CHEMBL2873)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mixed lineage kinase activity of indolocarbazole analogues.
Murakata C, Kaneko M, Gessner G, Angeles TS, Ator MA, O'Kane TM, McKenna BA, Thomas BA, Mathiasen JR, Saporito MS, Bozyczko-Coyne D, Hudkins RL.
Bioorg Med Chem Lett (2002) 12 : 147 -150
PubMed 11755341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.21 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288817 1 7.80
CHEMBL277817 1 7.70
CHEMBL288229 1 7.55
CHEMBL290352 CEP-1347 3.0 1 7.29
CHEMBL288816 1 7.05
CHEMBL36891 1 6.85
CHEMBL29709 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288817 IC50 = 16.0 nM 7.80
CHEMBL277817 IC50 = 20.0 nM 7.70
CHEMBL288229 IC50 = 28.0 nM 7.55
CHEMBL290352 CEP-1347 IC50 = 51.0 nM 7.29
CHEMBL288816 IC50 = 89.0 nM 7.05
CHEMBL36891 IC50 = 140.0 nM 6.85
CHEMBL29709 IC50 = 627.0 nM 6.20