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Assay Detail

CHEMBL1786489

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Binding
Binding affinity to Grp78 by isothermal titration calorimetric analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Endoplasmic reticulum chaperone BiP (CHEMBL1781865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivity.
Macias AT, Williamson DS, Allen N, Borgognoni J, Clay A, Daniels Z, Dokurno P, Drysdale MJ, Francis GL, Graham CJ, Howes R, Matassova N, Murray JB, Parsons R, Shaw T, Surgenor AE, Terry L, Wang Y, Wood M, Massey AJ.
J Med Chem (2011) 54 : 4034 -4041
PubMed 21526763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 6.08 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462871 1 7.00
CHEMBL470334 1 6.70
CHEMBL515570 1 6.46
CHEMBL516357 1 6.06
CHEMBL14830 ADENOSINE DIPHOSPHATE 0.5 1 5.42
CHEMBL516197 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462871 Kd = 100.0 nM 7.00
CHEMBL470334 Kd = 200.0 nM 6.70
CHEMBL515570 Kd = 350.0 nM 6.46
CHEMBL516357 Kd = 870.0 nM 6.06
CHEMBL14830 ADENOSINE DIPHOSPHATE Kd = 3830.0 nM 5.42
CHEMBL516197 Kd = 14140.0 nM 4.85