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Assay Detail

CHEMBL4135522

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

Binding
Displacement of FITC-GDA from recombinant canine Grp94 expressed in baculovirus infected Sf21 insect cells after 24 hrs by fluorescence polarization assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Endoplasmin (CHEMBL4748)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Resorcinol-Based Grp94-Selective Inhibitors.
Khandelwal A, Crowley VM, Blagg BSJ.
ACS Med Chem Lett (2017) 8 : 1013 -1018
PubMed 29057043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 20 7.36 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174059 1 8.10
CHEMBL4170618 1 7.89
CHEMBL4160774 1 7.89
CHEMBL4173418 1 7.82
CHEMBL4165495 1 7.77
CHEMBL4168598 1 7.70
CHEMBL4159747 1 7.68
CHEMBL4177418 1 7.54
CHEMBL4161657 1 7.54
CHEMBL4170382 1 7.52
CHEMBL4169566 1 7.51
CHEMBL4175693 1 7.47
CHEMBL4162694 1 7.40
CHEMBL4162283 1 7.23
CHEMBL4172951 1 7.22
CHEMBL4165074 1 7.16
CHEMBL4176780 1 6.11
CHEMBL4168916 1 5.00
CHEMBL4172281 1 -
CHEMBL4168694 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174059 Kd = 8.0 nM 8.10
CHEMBL4170618 Kd = 13.0 nM 7.89
CHEMBL4160774 Kd = 13.0 nM 7.89
CHEMBL4173418 Kd = 15.0 nM 7.82
CHEMBL4165495 Kd = 17.0 nM 7.77
CHEMBL4168598 Kd = 20.0 nM 7.70
CHEMBL4159747 Kd = 21.0 nM 7.68
CHEMBL4177418 Kd = 29.0 nM 7.54
CHEMBL4161657 Kd = 29.0 nM 7.54
CHEMBL4170382 Kd = 30.0 nM 7.52
CHEMBL4169566 Kd = 31.0 nM 7.51
CHEMBL4175693 Kd = 34.0 nM 7.47
CHEMBL4162694 Kd = 40.0 nM 7.40
CHEMBL4162283 Kd = 59.0 nM 7.23
CHEMBL4172951 Kd = 60.0 nM 7.22
CHEMBL4165074 Kd = 70.0 nM 7.16
CHEMBL4176780 Kd = 770.0 nM 6.11
CHEMBL4168916 Kd = 9890.0 nM 5.00
CHEMBL4172281 Kd > 10000.0 nM -
CHEMBL4168694 Kd > 100000.0 nM -