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Assay Detail

CHEMBL800659

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

Binding
Ability to displace [3H]9-cis-RA from Retinoid X receptor alpha in CV-1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of benzofused heterocyclic RXR modulators.
Gernert DL, Neel DA, Boehm MF, Leibowitz MD, Mais DA, Michellys PY, Rungta D, Reifel-Miller A, Grese TA.
Bioorg Med Chem Lett (2004) 14 : 2759 -2763
PubMed 15125928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.56 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430651 1 8.80
CHEMBL92447 1 8.80
CHEMBL88740 1 8.70
CHEMBL92243 1 8.57
CHEMBL93246 1 8.49
CHEMBL414218 1 8.40
CHEMBL92798 1 8.13
CHEMBL314745 1 7.53
CHEMBL91979 1 7.16
CHEMBL93571 1 6.88
CHEMBL264746 1 6.40
CHEMBL328507 1 6.19
CHEMBL421748 1 6.13
CHEMBL328072 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430651 Ki = 1.6 nM 8.80
CHEMBL92447 Ki = 1.6 nM 8.80
CHEMBL88740 Ki = 2.0 nM 8.70
CHEMBL92243 Ki = 2.7 nM 8.57
CHEMBL93246 Ki = 3.2 nM 8.49
CHEMBL414218 Ki = 4.0 nM 8.40
CHEMBL92798 Ki = 7.4 nM 8.13
CHEMBL314745 Ki = 29.6 nM 7.53
CHEMBL91979 Ki = 69.2 nM 7.16
CHEMBL93571 Ki = 131.0 nM 6.88
CHEMBL264746 Ki = 394.7 nM 6.40
CHEMBL328507 Ki = 648.0 nM 6.19
CHEMBL421748 Ki = 740.0 nM 6.13
CHEMBL328072 Ki = 2078.3 nM 5.68