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Assay Detail

CHEMBL864468

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Functional
Transcriptional activity against RARbeta2
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor beta (CHEMBL2008)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Lund BW, Piu F, Gauthier NK, Eeg A, Currier E, Sherbukhin V, Brann MR, Hacksell U, Olsson R.
J Med Chem (2005) 48 : 7517 -7519
PubMed 16302793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.61 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38 TRETINOIN 4.0 1 8.20
CHEMBL198997 1 8.00
CHEMBL197292 1 7.80
CHEMBL198794 1 7.80
CHEMBL69367 1 7.70
CHEMBL371684 1 7.60
CHEMBL198467 1 7.30
CHEMBL365798 1 7.20
CHEMBL425027 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38 TRETINOIN EC50 = 6.31 nM 8.20
CHEMBL198997 EC50 = 10.0 nM 8.00
CHEMBL197292 EC50 = 15.85 nM 7.80
CHEMBL198794 EC50 = 15.85 nM 7.80
CHEMBL69367 EC50 = 19.95 nM 7.70
CHEMBL371684 EC50 = 25.12 nM 7.60
CHEMBL198467 EC50 = 50.12 nM 7.30
CHEMBL365798 EC50 = 63.1 nM 7.20
CHEMBL425027 EC50 = 125.89 nM 6.90