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Assay Detail

CHEMBL5521990

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

Binding
Binding affinity to Keap1 (unknown origin) assessed as dissociation constant incubated for 60 mins by fluorescence polarization assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kelch-like ECH-associated protein 1 (CHEMBL2069156)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.
Zou J, Yan J, Lu Y, Yu Z, Zhang K, Han Q, Han D, Gai C, Chai X, Zhao Q, Zhuang C, Zou Y.
J Med Chem (2024) 67 : 4889 -4903
PubMed 38485922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 6.38 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561577 1 7.29
CHEMBL5556757 1 7.20
CHEMBL5567058 1 7.15
CHEMBL3134422 1 6.76
CHEMBL5550010 1 6.73
CHEMBL5561616 1 6.64
CHEMBL5558378 1 6.63
CHEMBL5562745 1 6.63
CHEMBL5562503 1 6.62
CHEMBL5532238 1 6.62
CHEMBL5560284 1 6.51
CHEMBL5561828 1 6.50
CHEMBL5567745 1 6.48
CHEMBL5566612 1 6.48
CHEMBL5559670 1 6.41
CHEMBL5563709 1 6.13
CHEMBL5555522 1 5.66
CHEMBL5557796 1 5.62
CHEMBL5558340 1 5.44
CHEMBL5557216 1 5.32
CHEMBL5559056 1 5.15
CHEMBL5564779 1 -
CHEMBL5559635 1 -
CHEMBL5562630 1 -
CHEMBL5564374 1 -
CHEMBL5568467 1 -
CHEMBL5561543 1 -
CHEMBL5555807 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561577 Kd = 51.0 nM 7.29
CHEMBL5556757 Kd = 63.0 nM 7.20
CHEMBL5567058 Kd = 71.0 nM 7.15
CHEMBL3134422 Kd = 172.0 nM 6.76
CHEMBL5550010 Kd = 185.0 nM 6.73
CHEMBL5561616 Kd = 229.0 nM 6.64
CHEMBL5558378 Kd = 232.0 nM 6.63
CHEMBL5562745 Kd = 235.0 nM 6.63
CHEMBL5562503 Kd = 237.0 nM 6.62
CHEMBL5532238 Kd = 238.0 nM 6.62
CHEMBL5560284 Kd = 306.0 nM 6.51
CHEMBL5561828 Kd = 313.0 nM 6.50
CHEMBL5567745 Kd = 334.0 nM 6.48
CHEMBL5566612 Kd = 328.0 nM 6.48
CHEMBL5559670 Kd = 386.0 nM 6.41
CHEMBL5563709 Kd = 747.0 nM 6.13
CHEMBL5555522 Kd = 2213.0 nM 5.66
CHEMBL5557796 Kd = 2414.0 nM 5.62
CHEMBL5558340 Kd = 3618.0 nM 5.44
CHEMBL5557216 Kd = 4834.0 nM 5.32
CHEMBL5559056 Kd = 7051.0 nM 5.15
CHEMBL5564779 Kd > 10000.0 nM -
CHEMBL5559635 Kd > 10000.0 nM -
CHEMBL5562630 Kd > 10000.0 nM -
CHEMBL5564374 Kd > 10000.0 nM -
CHEMBL5568467 Kd > 10000.0 nM -
CHEMBL5561543 Kd > 10000.0 nM -
CHEMBL5555807 Kd > 10000.0 nM -