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Assay Detail

CHEMBL4023964

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Binding
Binding affinity to human BAP-tagged AMPK alpha1/beta1/gamma1 by SPR assay
14
Total Activities
14
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

Publication

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO.
J Med Chem (2018) 61 : 2372 -2383
PubMed 29466005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 14 7.27 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891221 1 8.05
CHEMBL3970868 1 7.85
CHEMBL4105032 1 7.85
CHEMBL3986871 1 7.85
CHEMBL3959148 1 7.70
CHEMBL3891932 1 7.66
CHEMBL3931350 1 7.32
CHEMBL3928208 1 7.32
CHEMBL4097332 1 6.39
CHEMBL4079303 1 6.24
CHEMBL4087189 1 5.77
CHEMBL3921758 1 -
CHEMBL3985144 1 -
CHEMBL4059813 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891221 Kd = 9.0 nM 8.05
CHEMBL3970868 Kd = 14.0 nM 7.85
CHEMBL4105032 Kd = 14.0 nM 7.85
CHEMBL3986871 Kd = 14.0 nM 7.85
CHEMBL3959148 Kd = 20.0 nM 7.70
CHEMBL3891932 Kd = 22.0 nM 7.66
CHEMBL3931350 Kd = 48.0 nM 7.32
CHEMBL3928208 Kd = 48.0 nM 7.32
CHEMBL4097332 Kd = 410.0 nM 6.39
CHEMBL4079303 Kd = 580.0 nM 6.24
CHEMBL4087189 Kd = 1700.0 nM 5.77
CHEMBL3921758 Kd - -
CHEMBL3985144 Kd - -
CHEMBL4059813 Kd - -