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Assay Detail

CHEMBL806009

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

Binding
Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor RXR-beta (CHEMBL1870)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of retinoid X receptor-specific ligands that are potent inducers of adipogenesis in 3T3-L1 cells.
Canan Koch SS, Dardashti LJ, Cesario RM, Croston GE, Boehm MF, Heyman RA, Nadzan AM.
J Med Chem (1999) 42 : 742 -750
PubMed 10052980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.18 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162334 1 8.30
CHEMBL348797 1 8.22
CHEMBL423465 1 8.10
CHEMBL164902 1 7.85
CHEMBL166244 1 7.82
CHEMBL1023 BEXAROTENE 4.0 1 7.68
CHEMBL166201 1 7.24
CHEMBL165734 1 7.21
CHEMBL351943 1 7.04
CHEMBL3350249 1 6.92
CHEMBL98172 1 6.72
CHEMBL162005 1 6.55
CHEMBL164557 1 6.44
CHEMBL162827 1 6.21
CHEMBL163625 1 5.47
CHEMBL2110182 1 -
CHEMBL162876 1 -
CHEMBL348794 1 -
CHEMBL2110180 1 -
CHEMBL2110181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162334 Ki = 5.0 nM 8.30
CHEMBL348797 Ki = 6.0 nM 8.22
CHEMBL423465 Ki = 8.0 nM 8.10
CHEMBL164902 Ki = 14.0 nM 7.85
CHEMBL166244 Ki = 15.0 nM 7.82
CHEMBL1023 BEXAROTENE Ki = 21.0 nM 7.68
CHEMBL166201 Ki = 58.0 nM 7.24
CHEMBL165734 Ki = 61.0 nM 7.21
CHEMBL351943 Ki = 91.0 nM 7.04
CHEMBL3350249 Ki = 120.0 nM 6.92
CHEMBL98172 Ki = 191.0 nM 6.72
CHEMBL162005 Ki = 283.0 nM 6.55
CHEMBL164557 Ki = 363.0 nM 6.44
CHEMBL162827 Ki = 623.0 nM 6.21
CHEMBL163625 Ki = 3363.0 nM 5.47
CHEMBL2110182 Ki > 1000.0 nM -
CHEMBL162876 Ki > 1000.0 nM -
CHEMBL348794 Ki > 1000.0 nM -
CHEMBL2110180 Ki > 1000.0 nM -
CHEMBL2110181 Ki > 1000.0 nM -