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Assay Detail

CHEMBL2390480

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

Binding
Activation of recombinant AMPK alpha2beta1gamma1 (unknown origin) after 2 hrs by scintillation proximity assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

AMPK alpha2/beta1/gamma1 (CHEMBL3038455)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Development of Novel Alkene Oxindole Derivatives As Orally Efficacious AMP-Activated Protein Kinase Activators.
Yu LF, Li YY, Su MB, Zhang M, Zhang W, Zhang LN, Pang T, Zhang RT, Liu B, Li JY, Li J, Nan FJ.
ACS Med Chem Lett (2013) 4 : 475 -480
PubMed 24900695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.50 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242297 1 6.52
CHEMBL2386124 1 6.00
CHEMBL2386114 1 5.92
CHEMBL2386115 1 5.75
CHEMBL2386118 1 5.50
CHEMBL2385951 1 5.50
CHEMBL2386116 1 5.40
CHEMBL2386123 1 5.35
CHEMBL2386120 1 5.34
CHEMBL2385952 1 5.32
CHEMBL2386113 1 5.23
CHEMBL2386117 1 5.13
CHEMBL2386122 1 5.04
CHEMBL2386119 1 5.00
CHEMBL2386121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242297 EC50 = 300.0 nM 6.52
CHEMBL2386124 EC50 = 1000.0 nM 6.00
CHEMBL2386114 EC50 = 1200.0 nM 5.92
CHEMBL2386115 EC50 = 1800.0 nM 5.75
CHEMBL2386118 EC50 = 3200.0 nM 5.50
CHEMBL2385951 EC50 = 3200.0 nM 5.50
CHEMBL2386116 EC50 = 4000.0 nM 5.40
CHEMBL2386123 EC50 = 4500.0 nM 5.35
CHEMBL2386120 EC50 = 4600.0 nM 5.34
CHEMBL2385952 EC50 = 4800.0 nM 5.32
CHEMBL2386113 EC50 = 5900.0 nM 5.23
CHEMBL2386117 EC50 = 7400.0 nM 5.13
CHEMBL2386122 EC50 = 9200.0 nM 5.04
CHEMBL2386119 EC50 = 9900.0 nM 5.00
CHEMBL2386121 EC50 > 10000.0 nM -