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Assay Detail

CHEMBL3854711

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

Binding
Binding affinity to recombinant human AMPK alpha1/beta1/gamma1 by SPR binding assay
7
Total Activities
7
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

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.
Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J.
J Med Chem (2016) 59 : 8068 -8081
PubMed 27490827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.53 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3891221 1 8.05
CHEMBL3893781 1 7.64
CHEMBL3917068 1 7.04
CHEMBL3919304 1 6.82
CHEMBL3950160 1 5.75
CHEMBL752 ADENOSINE PHOSPHATE 4.0 1 5.43
CHEMBL3936376 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3891221 Kd = 9.0 nM 8.05
CHEMBL3893781 Kd = 22.7 nM 7.64
CHEMBL3917068 Kd = 90.2 nM 7.04
CHEMBL3919304 Kd = 149.8 nM 6.82
CHEMBL3950160 Kd = 1776.0 nM 5.75
CHEMBL752 ADENOSINE PHOSPHATE Kd = 3700.0 nM 5.43
CHEMBL3936376 Kd = 9948.0 nM 5.00