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Assay Detail

CHEMBL887724

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

Binding
Activity at RXRalpha by GAL4DNA cotransfection assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.
Lagu B, Lebedev R, Pio B, Yang M, Pelton PD.
Bioorg Med Chem Lett (2007) 17 : 3491 -3496
PubMed 17490875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 7.51 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248415 1 9.05
CHEMBL247220 1 8.85
CHEMBL246821 1 8.74
CHEMBL247401 1 8.64
CHEMBL399461 1 8.47
CHEMBL399326 1 8.30
CHEMBL246825 1 8.14
CHEMBL247402 1 8.00
CHEMBL246824 1 7.72
CHEMBL248016 1 7.55
CHEMBL410399 1 7.44
CHEMBL247000 1 7.42
CHEMBL246823 1 7.41
CHEMBL248236 1 7.34
CHEMBL400894 1 7.15
CHEMBL246210 1 6.94
CHEMBL247400 1 6.84
CHEMBL248414 1 6.70
CHEMBL246211 1 6.68
CHEMBL428406 1 6.44
CHEMBL399327 1 6.44
CHEMBL247849 1 6.28
CHEMBL246827 1 6.12
CHEMBL400868 1 -
CHEMBL247002 1 -
CHEMBL401053 1 -
CHEMBL247848 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248415 EC50 = 0.9 nM 9.05
CHEMBL247220 EC50 = 1.4 nM 8.85
CHEMBL246821 EC50 = 1.8 nM 8.74
CHEMBL247401 EC50 = 2.3 nM 8.64
CHEMBL399461 EC50 = 3.4 nM 8.47
CHEMBL399326 EC50 = 5.0 nM 8.30
CHEMBL246825 EC50 = 7.2 nM 8.14
CHEMBL247402 EC50 = 10.0 nM 8.00
CHEMBL246824 EC50 = 19.2 nM 7.72
CHEMBL248016 EC50 = 27.9 nM 7.55
CHEMBL410399 EC50 = 36.5 nM 7.44
CHEMBL247000 EC50 = 37.7 nM 7.42
CHEMBL246823 EC50 = 39.1 nM 7.41
CHEMBL248236 EC50 = 45.9 nM 7.34
CHEMBL400894 EC50 = 70.2 nM 7.15
CHEMBL246210 EC50 = 115.8 nM 6.94
CHEMBL247400 EC50 = 144.0 nM 6.84
CHEMBL248414 EC50 = 198.0 nM 6.70
CHEMBL246211 EC50 = 207.5 nM 6.68
CHEMBL428406 EC50 = 361.0 nM 6.44
CHEMBL399327 EC50 = 361.0 nM 6.44
CHEMBL247849 EC50 = 527.0 nM 6.28
CHEMBL246827 EC50 = 760.0 nM 6.12
CHEMBL400868 EC50 - -
CHEMBL247002 EC50 - -
CHEMBL401053 EC50 - -
CHEMBL247848 EC50 > 10000.0 nM -