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Assay Detail

CHEMBL4152129

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Binding
Binding affinity to Keap1 Kelch domain (unknown origin) by surface plasmon resonance assay
18
Total Activities
18
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

Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors.
Richardson BG, Jain AD, Potteti HR, Lazzara PR, David BP, Tamatam CR, Choma E, Skowron K, Dye K, Siddiqui Z, Wang YT, Krunic A, Reddy SP, Moore TW.
J Med Chem (2018) 61 : 8029 -8047
PubMed 30122040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 18 6.96 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237245 1 7.70
CHEMBL3632711 1 7.36
CHEMBL4166445 1 6.99
CHEMBL4174651 1 6.99
CHEMBL2402207 1 5.77
CHEMBL4166048 1 -
CHEMBL4173296 1 -
CHEMBL4162602 1 -
CHEMBL4169869 1 -
CHEMBL4159226 1 -
CHEMBL4174360 1 -
CHEMBL4176664 1 -
CHEMBL4176126 1 -
CHEMBL3600957 1 -
CHEMBL3632890 1 -
CHEMBL4160703 1 -
CHEMBL4171299 1 -
CHEMBL4166752 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237245 Kd = 20.0 nM 7.70
CHEMBL3632711 Kd = 44.0 nM 7.36
CHEMBL4166445 Kd = 103.0 nM 6.99
CHEMBL4174651 Kd = 102.0 nM 6.99
CHEMBL2402207 Kd = 1700.0 nM 5.77
CHEMBL4166048 Kd - -
CHEMBL4173296 Kd > 10000.0 nM -
CHEMBL4162602 Kd - -
CHEMBL4169869 Kd - -
CHEMBL4159226 Kd - -
CHEMBL4174360 Kd - -
CHEMBL4176664 Kd - -
CHEMBL4176126 Kd - -
CHEMBL3600957 Kd - -
CHEMBL3632890 Kd - -
CHEMBL4160703 Kd - -
CHEMBL4171299 Kd - -
CHEMBL4166752 Kd - -