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Assay Detail

CHEMBL5316718

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

Binding
Agonist activity at human GAL4-fused RXRalpha LBD expressed in human HEK293T cells cotransfected with pFR-Luc and pRL-SV40 assessed as increase in luciferase activity incubated for 16 hrs by Dual-Glo luciferase assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Rational Design of a New RXR Agonist Scaffold Enabling Single-Subtype Preference for RXRα, RXRβ, and RXRγ.
Adouvi G, Isigkeit L, López-García Ú, Chaikuad A, Marschner JA, Schubert-Zsilavecz M, Merk D.
J Med Chem (2023) 66 : 333 -344
PubMed 36533416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 5.61 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5415488 1 6.44
CHEMBL5430265 1 6.30
CHEMBL5415478 1 6.22
CHEMBL5398107 1 6.13
CHEMBL5417534 1 6.10
CHEMBL5395485 1 6.00
CHEMBL5436493 1 5.96
CHEMBL5411747 1 5.92
CHEMBL5397808 1 5.80
CHEMBL5420687 1 5.66
CHEMBL5412916 1 5.62
CHEMBL5420641 1 5.51
CHEMBL5416412 1 5.39
CHEMBL4864441 1 5.16
CHEMBL5423689 1 5.16
CHEMBL5415007 1 4.64
CHEMBL1545045 VALERENIC ACID 1 4.57
CHEMBL5411285 1 4.37
CHEMBL5403049 1 -
CHEMBL5433310 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5415488 EC50 = 360.0 nM 6.44
CHEMBL5430265 EC50 = 500.0 nM 6.30
CHEMBL5415478 EC50 = 600.0 nM 6.22
CHEMBL5398107 EC50 = 740.0 nM 6.13
CHEMBL5417534 EC50 = 800.0 nM 6.10
CHEMBL5395485 EC50 = 1000.0 nM 6.00
CHEMBL5436493 EC50 = 1100.0 nM 5.96
CHEMBL5411747 EC50 = 1200.0 nM 5.92
CHEMBL5397808 EC50 = 1600.0 nM 5.80
CHEMBL5420687 EC50 = 2200.0 nM 5.66
CHEMBL5412916 EC50 = 2400.0 nM 5.62
CHEMBL5420641 EC50 = 3100.0 nM 5.51
CHEMBL5416412 EC50 = 4100.0 nM 5.39
CHEMBL4864441 EC50 = 7000.0 nM 5.16
CHEMBL5423689 EC50 = 7000.0 nM 5.16
CHEMBL5415007 EC50 = 23000.0 nM 4.64
CHEMBL1545045 VALERENIC ACID EC50 = 27000.0 nM 4.57
CHEMBL5411285 EC50 = 43000.0 nM 4.37
CHEMBL5403049 EC50 > 100000.0 nM -
CHEMBL5433310 EC50 > 100000.0 nM -