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Assay Detail

CHEMBL5589300

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

Binding
Agonist activity at full length GST-tagged human THR-alpha LBD incubated for 1 hr in presence of fluorescein labeled SRC2-2 peptide by Lanthascreen TR-FRET assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thyroid hormone receptor alpha (CHEMBL1860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Preclinical Profile of ALG-055009, a Potent and Selective Thyroid Hormone Receptor Beta (THR-β) Agonist for the Treatment of MASH.
Vandyck K, McGowan DC, Luong XG, Stevens SK, Jekle A, Gupta K, Misner DL, Chanda S, Serebryany V, Welch M, Hu H, Lv Z, Williams C, Maskos K, Lammens A, Stoycheva AD, Lin TI, Blatt LM, Beigelman LN, Symons JA, Raboisson P, Deval J.
J Med Chem (2024) 67 : 14840 -14851
PubMed 39221768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.96 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5596442 1 7.10
CHEMBL5598346 1 6.54
CHEMBL5597482 1 6.44
CHEMBL3261331 RESMETIROM 4.0 1 6.03
CHEMBL5598441 1 5.75
CHEMBL5598332 1 5.67
CHEMBL5597989 1 5.66
CHEMBL5598543 1 5.63
CHEMBL5597130 1 4.79
CHEMBL5597744 1 -
CHEMBL5596618 1 -
CHEMBL5589816 1 -
CHEMBL5590206 1 -
CHEMBL5596268 1 -
CHEMBL5597882 1 -
CHEMBL5596341 1 -
CHEMBL5590707 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5596442 EC50 = 79.0 nM 7.10
CHEMBL5598346 EC50 = 291.0 nM 6.54
CHEMBL5597482 EC50 = 360.0 nM 6.44
CHEMBL3261331 RESMETIROM EC50 = 934.0 nM 6.03
CHEMBL5598441 EC50 = 1760.0 nM 5.75
CHEMBL5598332 EC50 = 2160.0 nM 5.67
CHEMBL5597989 EC50 = 2209.0 nM 5.66
CHEMBL5598543 EC50 = 2320.0 nM 5.63
CHEMBL5597130 EC50 = 16100.0 nM 4.79
CHEMBL5597744 EC50 > 50000.0 nM -
CHEMBL5596618 EC50 > 50000.0 nM -
CHEMBL5589816 EC50 > 50000.0 nM -
CHEMBL5590206 EC50 > 50000.0 nM -
CHEMBL5596268 EC50 > 50000.0 nM -
CHEMBL5597882 EC50 > 50000.0 nM -
CHEMBL5596341 EC50 > 50000.0 nM -
CHEMBL5590707 EC50 > 50000.0 nM -