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Assay Detail

CHEMBL3602663

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

Binding
Displacement of [3H]-1-MeHis-TRH from mouse TRH-R2 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thyrotropin-releasing hormone receptor 2 (CHEMBL3600274)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
Meena CL, Thakur A, Nandekar PP, Sangamwar AT, Sharma SS, Jain R.
Bioorg Med Chem (2015) 23 : 5641 -5653
PubMed 26216015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1472 PROTIRELIN 4.0 1 8.15
CHEMBL3601783 1 -
CHEMBL3601784 1 -
CHEMBL3601785 1 -
CHEMBL3601786 1 -
CHEMBL3600444 1 -
CHEMBL3600445 1 -
CHEMBL3600446 1 -
CHEMBL3600447 1 -
CHEMBL3600448 1 -
CHEMBL3600450 1 -
CHEMBL3601782 1 -
CHEMBL3601781 1 -
CHEMBL3600454 1 -
CHEMBL3600453 1 -
CHEMBL3600452 1 -
CHEMBL3600451 1 -
CHEMBL3600449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1472 PROTIRELIN IC50 = 7.0 nM 8.15
CHEMBL3601783 IC50 > 50000.0 nM -
CHEMBL3601784 IC50 > 50000.0 nM -
CHEMBL3601785 IC50 > 50000.0 nM -
CHEMBL3601786 IC50 > 50000.0 nM -
CHEMBL3600444 IC50 > 50000.0 nM -
CHEMBL3600445 IC50 > 50000.0 nM -
CHEMBL3600446 IC50 > 50000.0 nM -
CHEMBL3600447 IC50 > 50000.0 nM -
CHEMBL3600448 IC50 > 50000.0 nM -
CHEMBL3600450 IC50 > 50000.0 nM -
CHEMBL3601782 IC50 > 50000.0 nM -
CHEMBL3601781 IC50 > 50000.0 nM -
CHEMBL3600454 IC50 > 50000.0 nM -
CHEMBL3600453 IC50 > 50000.0 nM -
CHEMBL3600452 IC50 > 50000.0 nM -
CHEMBL3600451 IC50 > 50000.0 nM -
CHEMBL3600449 IC50 > 50000.0 nM -