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Assay Detail

CHEMBL3380010

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

Binding
Antagonist activity at maltose binding protein-tagged RBP4 (unknown origin) expressed in Escherichia coli assessed as inhibition of retinol-induced protein/transthyretin interaction by HTRF assay
35
Total Activities
35
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

Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Cioffi CL, Dobri N, Freeman EE, Conlon MP, Chen P, Stafford DG, Schwarz DM, Golden KC, Zhu L, Kitchen DB, Barnes KD, Racz B, Qin Q, Michelotti E, Cywin CL, Martin WH, Pearson PG, Johnson G, Petrukhin K.
J Med Chem (2014) 57 : 7731 -7757
PubMed 25210858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 8.89 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359024 1 9.92
CHEMBL1230001 1 9.81
CHEMBL3359022 1 9.75
CHEMBL3359023 1 9.63
CHEMBL3359017 1 9.54
CHEMBL3359014 1 9.53
CHEMBL3359019 1 9.47
CHEMBL3359015 1 9.32
CHEMBL3359005 1 9.26
CHEMBL3359028 1 9.08
CHEMBL3359020 1 8.81
CHEMBL3358470 1 8.58
CHEMBL3358466 1 8.50
CHEMBL3358465 1 8.40
CHEMBL3358464 1 8.28
CHEMBL3359026 1 8.28
CHEMBL3359025 1 8.17
CHEMBL3358463 1 8.17
CHEMBL3359029 1 8.08
CHEMBL3359011 1 8.08
CHEMBL3359027 1 8.04
CHEMBL3359013 1 -
CHEMBL3359012 1 -
CHEMBL3359016 1 -
CHEMBL3359018 1 -
CHEMBL3359010 1 -
CHEMBL3359009 1 -
CHEMBL3359021 1 -
CHEMBL3359008 1 -
CHEMBL3359007 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359024 IC50 = 0.121 nM 9.92
CHEMBL1230001 IC50 = 0.155 nM 9.81
CHEMBL3359022 IC50 = 0.179 nM 9.75
CHEMBL3359023 IC50 = 0.235 nM 9.63
CHEMBL3359017 IC50 = 0.285 nM 9.54
CHEMBL3359014 IC50 = 0.294 nM 9.53
CHEMBL3359019 IC50 = 0.34 nM 9.47
CHEMBL3359015 IC50 = 0.481 nM 9.32
CHEMBL3359005 IC50 = 0.554 nM 9.26
CHEMBL3359028 IC50 = 0.829 nM 9.08
CHEMBL3359020 IC50 = 1.55 nM 8.81
CHEMBL3358470 IC50 = 2.65 nM 8.58
CHEMBL3358466 IC50 = 3.13 nM 8.50
CHEMBL3358465 IC50 = 3.94 nM 8.40
CHEMBL3359026 IC50 = 5.26 nM 8.28
CHEMBL3358464 IC50 = 5.31 nM 8.28
CHEMBL3358463 IC50 = 6.8 nM 8.17
CHEMBL3359025 IC50 = 6.82 nM 8.17
CHEMBL3359029 IC50 = 8.34 nM 8.08
CHEMBL3359011 IC50 = 8.38 nM 8.08
CHEMBL3359027 IC50 = 9.19 nM 8.04
CHEMBL3358467 IC50 - -
CHEMBL3358468 IC50 - -
CHEMBL3358469 IC50 - -
CHEMBL3358471 IC50 - -
CHEMBL3359006 IC50 - -
CHEMBL3359007 IC50 - -
CHEMBL3359008 IC50 - -
CHEMBL3359021 IC50 - -
CHEMBL3359009 IC50 - -
CHEMBL3359010 IC50 - -
CHEMBL3359018 IC50 - -
CHEMBL3359016 IC50 - -
CHEMBL3359012 IC50 - -
CHEMBL3359013 IC50 - -