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Assay Detail

CHEMBL872293

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

Binding
Inhibitory constant against thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thyrotropin-releasing hormone receptor 2 (CHEMBL3875)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
Kaur N, Lu X, Gershengorn MC, Jain R.
J Med Chem (2005) 48 : 6162 -6165
PubMed 16162016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1472 PROTIRELIN 4.0 1 8.00
CHEMBL381666 1 -
CHEMBL198263 1 -
CHEMBL382714 1 -
CHEMBL382080 1 -
CHEMBL369944 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1472 PROTIRELIN Ki = 10.0 nM 8.00
CHEMBL381666 Ki > 100000.0 nM -
CHEMBL198263 Ki > 100000.0 nM -
CHEMBL382714 Ki > 100000.0 nM -
CHEMBL382080 Ki > 100000.0 nM -
CHEMBL369944 Ki > 100000.0 nM -