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Assay Detail

CHEMBL815539

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

Binding
Binding affinity for human tachykinin receptor 2 expressed in CHO cells using [125I]- NKA radioligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor.
MacKenzie AR, Marchington AP, Middleton DS, Newman SD, Selway CN, Terrett NK.
Bioorg Med Chem Lett (2003) 13 : 2211 -2215
PubMed 12798336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.14 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71918 1 8.20
CHEMBL71784 1 8.20
CHEMBL308901 1 8.19
CHEMBL69065 1 8.19
CHEMBL307338 1 8.18
CHEMBL71704 1 8.17
CHEMBL70157 1 8.17
CHEMBL305191 1 8.17
CHEMBL71394 1 8.15
CHEMBL304807 1 8.14
CHEMBL71644 1 8.14
CHEMBL71226 1 8.13
CHEMBL69889 1 8.12
CHEMBL68917 1 8.11
CHEMBL71647 1 8.11
CHEMBL305236 1 8.09
CHEMBL74127 1 8.08
CHEMBL71397 1 8.05
CHEMBL68440 1 8.05
CHEMBL69335 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71918 IC50 = 6.3 nM 8.20
CHEMBL71784 IC50 = 6.3 nM 8.20
CHEMBL308901 IC50 = 6.5 nM 8.19
CHEMBL69065 IC50 = 6.4 nM 8.19
CHEMBL307338 IC50 = 6.6 nM 8.18
CHEMBL71704 IC50 = 6.8 nM 8.17
CHEMBL70157 IC50 = 6.7 nM 8.17
CHEMBL305191 IC50 = 6.8 nM 8.17
CHEMBL71394 IC50 = 7.1 nM 8.15
CHEMBL304807 IC50 = 7.3 nM 8.14
CHEMBL71644 IC50 = 7.2 nM 8.14
CHEMBL71226 IC50 = 7.4 nM 8.13
CHEMBL69889 IC50 = 7.5 nM 8.12
CHEMBL68917 IC50 = 7.7 nM 8.11
CHEMBL71647 IC50 = 7.7 nM 8.11
CHEMBL305236 IC50 = 8.1 nM 8.09
CHEMBL74127 IC50 = 8.4 nM 8.08
CHEMBL71397 IC50 = 8.9 nM 8.05
CHEMBL68440 IC50 = 8.9 nM 8.05
CHEMBL69335 IC50 < 7.0 nM -