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Assay Detail

CHEMBL5738354

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Binding
In Vitro pAMPK1 Kinase Activation Assay: Compound effect on AMPK enzyme activation was determined in a cell-free format with a 12-point concentration curve. The ADP-Glo detection system was used to determine phosphorylation of a SAMS peptide substrate. Recombinant AMPK α1/β1/γ1 complex was pre-activated by phosphorylation with CAMKK2 followed by incubated with compound for 15 minutes prior to the SAMS phosphorylation reaction. Activity curves and EC50 values were fitted by interpolation to an ATP:ADP standard curve as indicated by the ADP-Glo manufacturer using Prism software.
ChEMBL ↗
162
Total Activities
53
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 (CHEMBL2111345) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

AMPK activators
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 54 9.03 10.30
kon 54 - -
k_off 54 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6048763 — — 3 10.30
CHEMBL5810593 — — 3 10.05
CHEMBL5836835 — — 3 10.00
CHEMBL5892252 — — 3 9.82
CHEMBL5771550 — — 3 9.64
CHEMBL5796255 — — 3 9.43
CHEMBL6009640 — — 3 9.40
CHEMBL5783632 — — 3 9.34
CHEMBL5891901 — — 3 9.30
CHEMBL5775914 — — 3 9.25
CHEMBL5784714 — — 3 9.24
CHEMBL5772530 — — 3 9.21
CHEMBL5813619 — — 3 9.20
CHEMBL5894957 — — 3 9.20
CHEMBL5881047 — — 3 9.19
CHEMBL5919560 — — 3 9.14
CHEMBL5825201 — — 3 9.12
CHEMBL5919095 — — 3 9.11
CHEMBL5919881 — — 3 9.10
CHEMBL5760186 — — 3 9.09
CHEMBL5992695 — — 3 9.08
CHEMBL5967863 — — 3 9.07
CHEMBL5805427 — — 3 9.07
CHEMBL5795930 — — 6 9.07
CHEMBL5770913 — — 3 9.05
CHEMBL5768406 — — 3 9.03
CHEMBL5761917 — — 3 9.03
CHEMBL5930657 — — 3 9.03
CHEMBL5983345 — — 3 9.02
CHEMBL5754808 — — 3 8.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6048763 — EC50 = 0.05 nM 10.30
CHEMBL5810593 — EC50 = 0.09 nM 10.05
CHEMBL5836835 — EC50 = 0.1 nM 10.00
CHEMBL5892252 — EC50 = 0.15 nM 9.82
CHEMBL5771550 — EC50 = 0.23 nM 9.64
CHEMBL5796255 — EC50 = 0.37 nM 9.43
CHEMBL6009640 — EC50 = 0.4 nM 9.40
CHEMBL5783632 — EC50 = 0.46 nM 9.34
CHEMBL5891901 — EC50 = 0.5 nM 9.30
CHEMBL5775914 — EC50 = 0.56 nM 9.25
CHEMBL5784714 — EC50 = 0.57 nM 9.24
CHEMBL5772530 — EC50 = 0.62 nM 9.21
CHEMBL5894957 — EC50 = 0.63 nM 9.20
CHEMBL5813619 — EC50 = 0.63 nM 9.20
CHEMBL5881047 — EC50 = 0.65 nM 9.19
CHEMBL5919560 — EC50 = 0.72 nM 9.14
CHEMBL5825201 — EC50 = 0.76 nM 9.12
CHEMBL5919095 — EC50 = 0.77 nM 9.11
CHEMBL5919881 — EC50 = 0.8 nM 9.10
CHEMBL5760186 — EC50 = 0.81 nM 9.09
CHEMBL5992695 — EC50 = 0.84 nM 9.08
CHEMBL5967863 — EC50 = 0.85 nM 9.07
CHEMBL5795930 — EC50 = 0.85 nM 9.07
CHEMBL5795930 — EC50 = 0.85 nM 9.07
CHEMBL5805427 — EC50 = 0.86 nM 9.07
CHEMBL5770913 — EC50 = 0.89 nM 9.05
CHEMBL5930657 — EC50 = 0.93 nM 9.03
CHEMBL5768406 — EC50 = 0.93 nM 9.03
CHEMBL5761917 — EC50 = 0.93 nM 9.03
CHEMBL5983345 — EC50 = 0.96 nM 9.02
CHEMBL5754808 — EC50 = 1.04 nM 8.98
CHEMBL5897987 — EC50 = 1.08 nM 8.97
CHEMBL6058212 — EC50 = 1.09 nM 8.96
CHEMBL5908554 — EC50 = 1.16 nM 8.94
CHEMBL5925731 — EC50 = 1.22 nM 8.91
CHEMBL5856248 — EC50 = 1.3 nM 8.89
CHEMBL6038711 — EC50 = 1.33 nM 8.88
CHEMBL5925602 — EC50 = 1.36 nM 8.87
CHEMBL5834613 — EC50 = 1.38 nM 8.86
CHEMBL5751541 — EC50 = 1.4 nM 8.85
CHEMBL5910201 — EC50 = 1.4 nM 8.85
CHEMBL5756252 — EC50 = 1.46 nM 8.84
CHEMBL5983956 — EC50 = 1.51 nM 8.82
CHEMBL5968839 — EC50 = 1.61 nM 8.79
CHEMBL5894992 — EC50 = 1.76 nM 8.75
CHEMBL5813373 — EC50 = 1.78 nM 8.75
CHEMBL5956230 — EC50 = 1.84 nM 8.73
CHEMBL5986738 — EC50 = 2.22 nM 8.65
CHEMBL5765610 — EC50 = 2.4 nM 8.62
CHEMBL5749579 — EC50 = 3.6 nM 8.44