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Assay Detail

CHEMBL770558

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

Functional
Ability to antagonise the contractile effects of the selective NK2 receptor agonist [B-ala8]NKA in the rabbit pulmonary artery (RPA)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

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
Kd 14 8.19 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71397 1 9.50
CHEMBL56835 1 9.10
CHEMBL71647 1 8.90
CHEMBL305236 1 8.60
CHEMBL74127 1 8.40
CHEMBL69889 1 8.40
CHEMBL68440 1 8.40
CHEMBL68917 1 8.30
CHEMBL71644 1 8.10
CHEMBL308901 1 7.70
CHEMBL71704 1 7.60
CHEMBL304807 1 7.30
CHEMBL70157 1 7.20
CHEMBL305191 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71397 Kd = 0.3162 nM 9.50
CHEMBL56835 Kd = 0.7943 nM 9.10
CHEMBL71647 Kd = 1.259 nM 8.90
CHEMBL305236 Kd = 2.512 nM 8.60
CHEMBL74127 Kd = 3.981 nM 8.40
CHEMBL69889 Kd = 3.981 nM 8.40
CHEMBL68440 Kd = 3.981 nM 8.40
CHEMBL68917 Kd = 5.012 nM 8.30
CHEMBL71644 Kd = 7.943 nM 8.10
CHEMBL308901 Kd = 19.95 nM 7.70
CHEMBL71704 Kd = 25.12 nM 7.60
CHEMBL304807 Kd = 50.12 nM 7.30
CHEMBL70157 Kd = 63.1 nM 7.20
CHEMBL305191 Kd = 79.43 nM 7.10