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Assay Detail

CHEMBL815486

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

Binding
Binding affinity towards Tachykinin receptor 2 in CHO cells using [3H]-neurokinin A as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-K receptor (CHEMBL2327)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and synthesis of novel NK1/NK2 dual antagonists.
Reichard GA, Ball ZT, Aslanian R, Anthes JC, Shih NY, Piwinski JJ.
Bioorg Med Chem Lett (2000) 10 : 2329 -2332
PubMed 11055349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.48 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308148 SAREDUTANT 3.0 1 9.30
CHEMBL72930 1 8.15
CHEMBL309087 1 7.68
CHEMBL405129 1 7.47
CHEMBL407749 1 7.47
CHEMBL293432 1 6.91
CHEMBL76334 1 6.45
CHEMBL311387 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308148 SAREDUTANT Ki = 0.5 nM 9.30
CHEMBL72930 Ki = 7.0 nM 8.15
CHEMBL309087 Ki = 21.0 nM 7.68
CHEMBL405129 Ki = 34.0 nM 7.47
CHEMBL407749 Ki = 34.0 nM 7.47
CHEMBL293432 Ki = 122.0 nM 6.91
CHEMBL76334 Ki = 358.0 nM 6.45
CHEMBL311387 Ki = 397.0 nM 6.40