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Assay Detail

CHEMBL829011

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Functional
Agonist activity towards thyroid hormone receptor expressed in human HepG2 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 7 — Homologous single protein target
Curated By Expert

Target

Thyroid hormone receptor (CHEMBL2111462)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Novel heterocyclic thyromimetics.
Haning H, Woltering M, Mueller U, Schmidt G, Schmeck C, Voehringer V, Kretschmer A, Pernerstorfer J.
Bioorg Med Chem Lett (2005) 15 : 1835 -1840
PubMed 15780617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 8.07 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182339 1 9.70
CHEMBL361162 1 9.30
CHEMBL360137 1 8.92
CHEMBL183176 1 8.52
CHEMBL183050 1 8.40
CHEMBL359647 1 8.40
CHEMBL183122 1 8.40
CHEMBL183000 1 8.11
CHEMBL183851 1 8.10
CHEMBL182430 1 8.10
CHEMBL183863 1 7.96
CHEMBL183727 1 7.82
CHEMBL183057 1 7.82
CHEMBL180952 1 7.75
CHEMBL183565 1 7.64
CHEMBL183829 1 7.14
CHEMBL360774 1 6.94
CHEMBL180819 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182339 EC50 = 0.2 nM 9.70
CHEMBL361162 EC50 = 0.5 nM 9.30
CHEMBL360137 EC50 = 1.2 nM 8.92
CHEMBL183176 EC50 = 3.0 nM 8.52
CHEMBL183050 EC50 = 4.0 nM 8.40
CHEMBL359647 EC50 = 4.0 nM 8.40
CHEMBL183122 EC50 = 4.0 nM 8.40
CHEMBL183000 EC50 = 7.8 nM 8.11
CHEMBL183851 EC50 = 8.0 nM 8.10
CHEMBL182430 EC50 = 8.0 nM 8.10
CHEMBL183863 EC50 = 11.0 nM 7.96
CHEMBL183727 EC50 = 15.0 nM 7.82
CHEMBL183057 EC50 = 15.0 nM 7.82
CHEMBL180952 EC50 = 18.0 nM 7.75
CHEMBL183565 EC50 = 23.0 nM 7.64
CHEMBL183829 EC50 = 72.0 nM 7.14
CHEMBL360774 EC50 = 115.0 nM 6.94
CHEMBL180819 EC50 = 495.0 nM 6.30