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Assay Detail

CHEMBL1804183

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

Binding
Binding affinity to His-tagged recombinant human sRBP expressed in Escherichia coli BL21(DE3) assessed as apparent dissociation constant after 5 mins by fluorescence spectrophotometric analysis
8
Total Activities
8
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

Retinol-binding protein 4 (CHEMBL3100)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fenretinide derivatives act as disrupters of interactions of serum retinol binding protein (sRBP) with transthyretin and the sRBP receptor.
Campos-Sandoval JA, Redondo C, Kinsella GK, Pal A, Jones G, Eyre GS, Hirst SC, Findlay JB.
J Med Chem (2011) 54 : 4378 -4387
PubMed 21591606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 6.75 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802450 1 7.01
CHEMBL1801542 1 6.88
CHEMBL7301 FENRETINIDE 3.0 1 6.81
CHEMBL1803043 1 6.75
CHEMBL986 RETINOL 4.0 1 6.74
CHEMBL60405 1 6.67
CHEMBL1802454 1 6.64
CHEMBL58106 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802450 Kd = 98.0 nM 7.01
CHEMBL1801542 Kd = 131.0 nM 6.88
CHEMBL7301 FENRETINIDE Kd = 156.0 nM 6.81
CHEMBL1803043 Kd = 178.0 nM 6.75
CHEMBL986 RETINOL Kd = 182.0 nM 6.74
CHEMBL60405 Kd = 214.0 nM 6.67
CHEMBL1802454 Kd = 227.0 nM 6.64
CHEMBL58106 Kd = 333.0 nM 6.48