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Assay Detail

CHEMBL4414348

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

Binding
Binding affinity to recombinant RXRalpha (unknown origin) by isothermal titration calorimetry
6
Total Activities
6
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

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tuning Nuclear Receptor Selectivity of Wy14,643 towards Selective Retinoid X Receptor Modulation.
Pollinger J, Gellrich L, Schierle S, Kilu W, Schmidt J, Kalinowsky L, Ohrndorf J, Kaiser A, Heering J, Proschak E, Merk D.
J Med Chem (2019) 62 : 2112 -2126
PubMed 30702885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 6.42 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4558880 1 7.02
CHEMBL1023 BEXAROTENE 4.0 1 6.68
CHEMBL4575123 1 6.46
CHEMBL4518775 1 6.06
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.89
CHEMBL459972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4558880 Kd = 95.0 nM 7.02
CHEMBL1023 BEXAROTENE Kd = 210.0 nM 6.68
CHEMBL4575123 Kd = 350.0 nM 6.46
CHEMBL4518775 Kd = 880.0 nM 6.06
CHEMBL295416 PIRINIXIC ACID Kd = 1280.0 nM 5.89
CHEMBL459972 Kd - -