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Assay Detail

CHEMBL4611425

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

Binding
Binding affinity to Keap1 (unknown origin) by SPR assay
10
Total Activities
10
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

Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.
Ma B, Lucas B, Capacci A, Lin EY, Jones JH, Dechantsreiter M, Enyedy I, Marcotte D, Xiao G, Li B, Richter K.
Bioorg Med Chem Lett (2020) 30 : 126852 -126852
PubMed 31898999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 8.20 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644995 1 10.15
CHEMBL4643134 1 9.15
CHEMBL4633657 1 9.06
CHEMBL4634531 1 8.72
CHEMBL4642419 1 8.57
CHEMBL4635041 1 7.87
CHEMBL4640695 1 7.69
CHEMBL4635896 1 7.25
CHEMBL4637979 1 7.22
CHEMBL2402207 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644995 Kd = 0.07 nM 10.15
CHEMBL4643134 Kd = 0.7 nM 9.15
CHEMBL4633657 Kd = 0.88 nM 9.06
CHEMBL4634531 Kd = 1.91 nM 8.72
CHEMBL4642419 Kd = 2.7 nM 8.57
CHEMBL4635041 Kd = 13.5 nM 7.87
CHEMBL4640695 Kd = 20.5 nM 7.69
CHEMBL4635896 Kd = 56.0 nM 7.25
CHEMBL4637979 Kd = 59.5 nM 7.22
CHEMBL2402207 Kd = 500.0 nM 6.30