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Assay Detail

CHEMBL799802

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

Binding
Binding affinity to retinoic acid receptor alpha using [3H]CD 367 as radioligand
25
Total Activities
25
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 alpha (CHEMBL2055)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Charpentier B, Bernardon JM, Eustache J, Millois C, Martin B, Michel S, Shroot B.
J Med Chem (1995) 38 : 4993 -5006
PubMed 8544175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.26 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36768 1 8.28
CHEMBL38 TRETINOIN 4.0 1 7.80
CHEMBL275311 1 7.68
CHEMBL74826 1 6.89
CHEMBL356326 1 6.38
CHEMBL146449 1 6.34
CHEMBL25361 1 6.24
CHEMBL146646 1 6.21
CHEMBL357917 1 6.16
CHEMBL348449 1 6.08
CHEMBL345022 1 5.98
CHEMBL1265 ADAPALENE 4.0 1 5.96
CHEMBL345298 1 5.95
CHEMBL421773 1 5.94
CHEMBL147545 1 5.30
CHEMBL146092 1 5.19
CHEMBL1180 O-DEMETHYLATED ADAPALENE 1 5.19
CHEMBL342051 1 5.07
CHEMBL357603 1 -
CHEMBL422490 1 -
CHEMBL148231 1 -
CHEMBL74218 1 -
CHEMBL149366 1 -
CHEMBL145911 1 -
CHEMBL146636 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36768 Ki = 5.3 nM 8.28
CHEMBL38 TRETINOIN Ki = 16.0 nM 7.80
CHEMBL275311 Ki = 21.0 nM 7.68
CHEMBL74826 Ki = 130.0 nM 6.89
CHEMBL356326 Ki = 420.0 nM 6.38
CHEMBL146449 Ki = 460.0 nM 6.34
CHEMBL25361 Ki = 580.0 nM 6.24
CHEMBL146646 Ki = 610.0 nM 6.21
CHEMBL357917 Ki = 695.0 nM 6.16
CHEMBL348449 Ki = 834.0 nM 6.08
CHEMBL345022 Ki = 1056.0 nM 5.98
CHEMBL1265 ADAPALENE Ki = 1100.0 nM 5.96
CHEMBL345298 Ki = 1120.0 nM 5.95
CHEMBL421773 Ki = 1144.0 nM 5.94
CHEMBL147545 Ki = 5000.0 nM 5.30
CHEMBL146092 Ki = 6500.0 nM 5.19
CHEMBL1180 O-DEMETHYLATED ADAPALENE Ki = 6500.0 nM 5.19
CHEMBL342051 Ki = 8500.0 nM 5.07
CHEMBL357603 Ki > 10000.0 nM -
CHEMBL422490 Ki > 10000.0 nM -
CHEMBL148231 Ki > 10000.0 nM -
CHEMBL74218 Ki > 10000.0 nM -
CHEMBL149366 Ki > 10000.0 nM -
CHEMBL145911 Ki > 10000.0 nM -
CHEMBL146636 Ki > 10000.0 nM -