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Assay Detail

CHEMBL5228924

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

Binding
Binding affinity to biotinylated USP5 zinc finger ubiquitin binding domain (171 to 290 residues) (unknown origin) expressed in Escherichia coli by surface plasmon resonance assay
56
Total Activities
56
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

Ubiquitin carboxyl-terminal hydrolase 5 (CHEMBL6158)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship of USP5 Inhibitors.
Mann MK, Zepeda-Velázquez CA, González-Álvarez H, Dong A, Kiyota T, Aman AM, Loppnau P, Li Y, Wilson B, Arrowsmith CH, Al-Awar R, Harding RJ, Schapira M.
J Med Chem (2021) 64 : 15017 -15036
PubMed 34648286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 56 4.54 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5278336 1 5.55
CHEMBL5266862 1 5.51
CHEMBL5267510 1 5.16
CHEMBL5270943 1 5.16
CHEMBL5273203 1 5.10
CHEMBL5267112 1 5.05
CHEMBL5271929 1 5.05
CHEMBL5276559 1 4.92
CHEMBL5274579 1 4.89
CHEMBL5283754 1 4.80
CHEMBL5266393 1 4.75
CHEMBL5277702 1 4.72
CHEMBL5281654 1 4.68
CHEMBL5280865 1 4.68
CHEMBL5265979 1 4.66
CHEMBL5273795 1 4.66
CHEMBL5285627 1 4.64
CHEMBL5268432 1 4.60
CHEMBL5269269 1 4.51
CHEMBL5282322 1 4.51
CHEMBL5272566 1 4.48
CHEMBL5266658 1 4.47
CHEMBL5268053 1 4.47
CHEMBL5282155 1 4.42
CHEMBL5290467 1 4.41
CHEMBL5266727 1 4.40
CHEMBL5290098 1 4.38
CHEMBL5290717 1 4.35
CHEMBL5286035 1 4.33
CHEMBL5270273 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5278336 Kd = 2800.0 nM 5.55
CHEMBL5266862 Kd = 3100.0 nM 5.51
CHEMBL5270943 Kd = 7000.0 nM 5.16
CHEMBL5267510 Kd = 7000.0 nM 5.16
CHEMBL5273203 Kd = 8000.0 nM 5.10
CHEMBL5267112 Kd = 9000.0 nM 5.05
CHEMBL5271929 Kd = 9000.0 nM 5.05
CHEMBL5276559 Kd = 12000.0 nM 4.92
CHEMBL5274579 Kd = 13000.0 nM 4.89
CHEMBL5283754 Kd = 16000.0 nM 4.80
CHEMBL5266393 Kd = 18000.0 nM 4.75
CHEMBL5277702 Kd = 19000.0 nM 4.72
CHEMBL5281654 Kd = 21000.0 nM 4.68
CHEMBL5280865 Kd = 21000.0 nM 4.68
CHEMBL5273795 Kd = 22000.0 nM 4.66
CHEMBL5265979 Kd = 22000.0 nM 4.66
CHEMBL5285627 Kd = 23000.0 nM 4.64
CHEMBL5268432 Kd = 25000.0 nM 4.60
CHEMBL5269269 Kd = 31000.0 nM 4.51
CHEMBL5282322 Kd = 31000.0 nM 4.51
CHEMBL5272566 Kd = 33000.0 nM 4.48
CHEMBL5266658 Kd = 34000.0 nM 4.47
CHEMBL5268053 Kd = 34000.0 nM 4.47
CHEMBL5282155 Kd = 38000.0 nM 4.42
CHEMBL5290467 Kd = 39000.0 nM 4.41
CHEMBL5266727 Kd = 40000.0 nM 4.40
CHEMBL5290098 Kd = 42000.0 nM 4.38
CHEMBL5290717 Kd = 45000.0 nM 4.35
CHEMBL5286035 Kd = 47000.0 nM 4.33
CHEMBL5270273 Kd = 54000.0 nM 4.27
CHEMBL5289065 Kd = 59000.0 nM 4.23
CHEMBL5282742 Kd = 61000.0 nM 4.21
CHEMBL5290299 Kd = 61000.0 nM 4.21
CHEMBL5279202 Kd = 67000.0 nM 4.17
CHEMBL5282232 Kd = 71000.0 nM 4.15
CHEMBL4440506 Kd = 80000.0 nM 4.10
CHEMBL5274675 Kd = 79000.0 nM 4.10
CHEMBL5273898 Kd = 80000.0 nM 4.10
CHEMBL5268349 Kd = 82000.0 nM 4.09
CHEMBL5283991 Kd = 87000.0 nM 4.06
CHEMBL5270844 Kd = 90000.0 nM 4.05
CHEMBL5285781 Kd = 92000.0 nM 4.04
CHEMBL5273690 Kd = 94000.0 nM 4.03
CHEMBL5284285 Kd = 130000.0 nM -
CHEMBL5269641 Kd = 270000.0 nM -
CHEMBL5267700 Kd = 110000.0 nM -
CHEMBL5275351 Kd = 170000.0 nM -
CHEMBL5282333 Kd = 150000.0 nM -
CHEMBL5276984 Kd = 150000.0 nM -
CHEMBL5285743 Kd = 130000.0 nM -